Target family: Histamine receptors (type: gpcr)
Target: H<sub>1</sub> receptor

Ligand: 2-(2-thiazolyl)ethanamine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.34 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: 2-(3-bromophenyl)histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: 2-(3-chlorophenyl)histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: 2-(3-iodophenyl)histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: 2-pyridylethylamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.7 pKi
Reference (Journal): Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
Published in: Eur J Biochem

Ligand: 9-OH-risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-349821 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: ABT-239 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Published in: J Pharmacol Exp Ther

Ligand: alimemazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 9.140000343322754 pKi
Reference (Journal): Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay.
Published in: Jpn J Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 9.300000190734863 pKi
Reference (Journal): Novel ligands for the human histamine H1 receptor: synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1,2,3,4-tetrahydronaphthalenes.
Published in: Bioorg Med Chem

Ligand: aripiprazole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Median affinity: 7.5 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: arpromidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: arpromidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: asenapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009), EMA (2010)
Median affinity: 9.8 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: astemizole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.520000457763672 pKi
Reference (Journal): Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.
Published in: J Med Chem

Ligand: AZD3778 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): The discovery of CCR3/H1 dual antagonists with reduced hERG risk.
Published in: Bioorg Med Chem Lett

Ligand: azelastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Published in: J Med Chem

Ligand: bilastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2010)
Primary target: no
Median affinity: 7.190000057220459 pKi
Reference (Journal): Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity.
Published in: Drugs R D

Ligand: BU-E 47 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: cetirizine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 8.199999809265137 pKi
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: (+)-chlorpheniramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: (+)-chlorpheniramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: (-)-chlorpheniramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: chlorpheniramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: yes
Median affinity: 8.149999618530273 pKi
Reference (Journal): The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Published in: J Med Chem

Ligand: chlorpromazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 8.2 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: chlorprothixene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.430000305175781 pKi
Reference (Journal): Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.
Published in: Bioorg Med Chem Lett

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: clemastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 10.3100004196167 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: conessine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: cyclizine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (date unknown)
Primary target: yes
Median affinity: 8.350000381469727 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: cyproheptadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 10.199999809265137 pKi
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: desloratadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2001)
Primary target: yes
Median affinity: 9.010000228881836 pKi
Reference (Journal): Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Published in: Bioorg Med Chem Lett

Ligand: dimethylhistaprodifen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: diphenhydramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1946)
Primary target: yes
Median affinity: 7.900000095367432 pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: dosulepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.
Published in: Cell Mol Neurobiol

Ligand: doxepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1969)
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: epinastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization.
Published in: J Pharmacol Sci

Ligand: fexofenadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 7.570000171661377 pKi
Reference (Journal): Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Published in: Bioorg Med Chem Lett

Ligand: fluphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 7.7 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: fluspirilene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7.9 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
Published in: Eur J Biochem

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: histaprodifen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: hydroxyzine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
Published in: Mol Pharmacol

Ligand: (+)-cis-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: impromidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: INCB-38579 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: (R)-cetirizine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: FDA (2007)
Primary target: yes
Median affinity: 8.5 pKi
Reference (Journal): Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
Published in: Eur J Biochem

Ligand: (S)-cetirizine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKi
Reference (Journal): Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
Published in: Eur J Biochem

Ligand: (+)-trans-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: (-)-trans-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-39758979 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: ketotifen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1999)
Primary target: yes
Median affinity: 8.600000381469727 pKi
Reference (Journal): Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.
Published in: Bioorg Med Chem

Ligand: loratadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity: 7.429999828338623 pKi
Reference (Journal): Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.
Published in: J Med Chem

Ligand: loxapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2013)
Median affinity: 8.2 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: mepyramine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
Published in: Eur J Biochem

Ligand: mepyramine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: methylhistaprodifen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: mizolastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2003)
Primary target: yes
Median affinity: 8.569999694824219 pKi
Reference (Journal): Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.
Published in: Bioorg Med Chem Lett

Ligand: mizolastine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2003)
Primary target: no
Median affinity: 7.329999923706055 pIC50
Reference (Journal): In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent.
Published in: Arzneimittelforschung

Ligand: MK-0249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: molindone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity: 5.7 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: olanzapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: oxo-arpromidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.5 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: perphenazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 8.1 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: pimozide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Median affinity: 6.2 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: pipamperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: pitolisant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2016), FDA (2019)
Primary target: no
Median affinity: 5.78000020980835 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: (±)-cis-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: (±)-cis-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: (±)-trans-H2-PAT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: promethazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1951)
Primary target: yes
Median affinity: 9.619999885559082 pKi
Reference (Journal): Novel ligands for the human histamine H1 receptor: synthesis, pharmacology, and comparative molecular field analysis studies of 2-dimethylamino-5-(6)-phenyl-1,2,3,4-tetrahydronaphthalenes.
Published in: Bioorg Med Chem

Ligand: quetiapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: quetiapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: rupatadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2007)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF).
Published in: J Pharmacol Exp Ther

Ligand: rupatadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: UK (2007)
Primary target: yes
Median affinity: 8.40999984741211 pIC50
Reference (Journal): Designed multiple ligands. An emerging drug discovery paradigm.
Published in: J Med Chem

Ligand: (S)-dimetindene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.159999847412109 pKi
Reference (Journal): Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
Published in: J Med Chem

Ligand: sertindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6.9 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: sertindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6.9 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: ST-1006 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: [11C]doxepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species.
Published in: Nucl Med Biol

Ligand: [11C]pyrilamine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]pyrilamine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]pyrilamine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: [3H]pyrilamine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Structure of the human histamine H1 receptor gene.
Published in: Biochem J

Ligand: [3H]pyrilamine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: terfenadine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA
Primary target: yes
Median affinity: 7.400000095367432 pKi
Reference (Journal): Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Published in: Bioorg Med Chem Lett

Ligand: thioridazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity: 7.7 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: thiothixene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity: 8.4 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: trifluoperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 7.2 pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: tripelennamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1948)
Primary target: yes
Median affinity: 8 pKd
Reference (Journal): Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
Published in: J Med Chem

Ligand: tripelennamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1948)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
Published in: J Med Chem

Ligand: triprolidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
Published in: Eur J Biochem

Ligand: triprolidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity:  pKi
Reference (Journal): A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Published in: J Pharmacol Exp Ther

Ligand: UR-PG131A (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: UR-PG146 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: UR-PG153 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: UR-PG55B (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: vilazodone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2011)
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Published in: J Med Chem

Ligand: ziprasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2001)
Median affinity:  pKi
Reference (Journal): H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
Published in: Neuropsychopharmacology

Ligand: ziprasidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2001)
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 9.2 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)