@entity3826 ( @entity3827 ) stimulates @entity2124 ( @entity2124 ) release via @entity935 D2 receptors ( @entity1633 ). There is no specific study assessing the relationship between @entity3827 pharmacokinetic (PK) and the pharmacodynamic (PD) response e.g. @entity2124 release. The objective of the study is the PK-PD modelling of @entity3827 in healthy subjects. This is a randomized crossover study with s.c. administration of 5, 10, and 20 micro g/kg of @entity3827 in 18 healthy subjects. @entity3827 concentrations were modelled according to both a bi-compartmental model with zero-order absorption and a bi-compartmental model with first-order absorption. PK-PD relationship was modelled in accordance with the Emax Hill equation using plasma concentrations of @entity3827 calculated according to the bi-compartmental model with zero-order absorption. Modelled parameters were very similar to the experimental parameters. PK of @entity3827 was linear and there was no significant difference between the tested doses for AUC0--> infinity and Cmax (normalised to the dose 1 micro g/kg), @entity8034 . These parameters expressed as mean (CV%: SD/mean) were: 17.2 (26.9) ng/mL.min, 0.26 (33.3) ng/mL, 17.1 (54.2) and 45.2 (20.6) min, respectively (n = 53). An anticlockwise hysteresis loop (effect function of @entity3827 plasma concentration) appeared for each dose and each subject. The predicted and measured @entity2124 concentrations for all subjects and times were similar whatever the dose (P > 0.27). Emax values were 246 (121), 180 (107), 205 (139) ng/mL, respectively, and EC50 were 0.98 (48.1), 1.70 (62.3), 3.67 (65.2) ng/mL, respectively at dose 5, 10, and 20 micro g/kg ( @entity14567 ). @entity3827 and @entity2124 concentrations were predicted with good accuracy using bi-compartmental with zero-order absorption PK model and sigmoid Emax PD model, respectively.

Pharmacokinetic-pharmacodynamic study of XXXX 's effect on @entity2124 secretion in healthy subjects.

@entity8034 :: ('9173', 'Gene') :: ['t1/2alpha and t1/2beta'] @entity935 :: ('MESH:D004298', 'Chemical') :: ['dopamine'] @entity14567 :: ('4820', 'Gene') :: ['P < 10-4'] @entity2124 :: ('2688', 'Gene') :: ['GH', 'growth hormone'] @entity3826 :: ('MESH:D001058', 'Chemical') :: ['Apomorphine'] @entity3827 :: ('CHEBI:53704', 'Chemical') :: ['APO'] @entity1633 :: ('1813', 'Gene') :: ['DRD2']
@entity3826 :: (MESH:D001058,Chemical) :: ['apomorphine']
