bluuebunny/crossref_metadata_2025_split huggingface dataset:
A Review of the Pharmacological and Clinical Profile of Mirtazapine
Authors: Anttila Sami A. K. , Leinonen Esa V. J. 
Published: August 2010

ABSTRACTThe novel antidepressant mirtazapine has a dual mode of action. It is a noradrenergic and specific serotonergic antidepressant (NaSSA) that acts by antagonizing the adrenergic α2‐autoreceptors and α2‐heteroreceptors as well as by blocking 5‐HT2and 5‐HT3receptors. It enhances, therefore, the release of norepinephrine and 5‐HT1A‐mediated serotonergic transmission. This dual mode of action may conceivably be responsible for mirtazapine's rapid onset of action.Mirtazapine is extensively metabolized in the liver. The cytochrome (CYP) P450 isoenzymes CYP1A2, CYP2D6, and CYP3A4 are mainly responsible for its metabolism. Using once daily dosing, steady‐state concentrations are reached after 4 days in adults and 6 days in the elderly.In vitrostudies suggest that mirtazapine is unlikely to cause clinically significant drug‐drug interactions. Dry mouth, sedation, and increases in appetite and body weight are the most common adverse effects. In contrast to selective serotonin reuptake inhibitors (SSRIs), mirtazapine has no sexual side effects.The antidepressant efficacy of mirtazapine was established in several placebo‐controlled trials. In major depression, its efficacy is comparable to that of amitriptyline, clomipramine, doxepin, fluoxetine, paroxetine, citalopram, or venlafaxine. Mirtazapine also appears to be useful in patients suffering from depression comorbid with anxiety symptoms and sleep disturbance. It seems to be safe and effective during long‐term use.
Galanin: Neurobiologic Mechanisms and Therapeutic Potential for Alzheimer's Disease
Authors: Counts Scott E. , Perez Sylvia E. , Kahl Ulrika , Bartfai Tamas , Bowser Robert P. , Deecher Darlene C. , Mash Deborah C. , Crawley Jacqueline N. , Mufson Elliott J. 
Published: August 2010

ABSTRACTThe neuropeptide galanin (GAL) is widely distributed in the mammalian CNS. Several lines of evidence suggest that GAL may play a critical role in cognitive processes such as memory and attention through an inhibitory modulation of cholinergic basal forebrain activity. Furthermore, GAL fibers hyperinnervate remaining cholinergic basal forebrain neurons in Alzheimer's disease (AD). This suggests that GAL activity impacts cholinergic dysfunction in advanced AD. Pharmacological andin vitroautoradiographic studies indicate the presence of heterogeneous populations of GAL receptor (GALR) sites in the basal forebrain which bind GAL with both high and low affinity. Interestingly, we have recently observed that GALR binding sites increase in the anterior basal forebrain in late‐stage AD. Three G protein‐coupled GALRs have been identified to date that signal through a diverse array of effector pathwaysin vitro, including adenylyl cyclase inhibition and phospholipase C activation. The repertoire and distribution of GALR expression in the basal forebrain remains unknown, as does the nature of GAL and GALR plasticity in the AD basal forebrain. Recently, GAL knockout and overexpressing transgenic mice have been generated to facilitate our understanding of GAL activity in basal forebrain function. GAL knockout mice result in fewer cholinergic basal forebrain neurons and memory deficits. On the other hand, mice overexpressing GAL display hyperinnervation of basal forebrain and memory deficits. These data highlight the need to explore further the putative mechanisms by which GAL signaling might be beneficial or deleterious for cholinergic cell survival and activity within basal forebrain. This information will be critical to understanding whether pharmacological manipulation of GALRs would be effective for the amelioration of cognitive deficits in AD.
(S)‐3,5‐DHPG: A Review
Authors: Wiśniewski Konstanty , Car Halina 
Published: August 2010

ABSTRACT3,5‐dihydroxyphenylglycine (3,5‐DHPG) was the first agonist shown to be group I metabotropic glutamate receptor selective with its agonist effects residing exclusively in the S‐isomer. Some results suggest that (S)‐3,5‐DHPG may be a partial agonist of mGluR1aand mGluR5ain neurons and astrocytes. It has been reported that (S)‐3,5‐DHPG can, under certain conditions, interact with NMDA receptors. (S)‐3,5‐DHPG exerts different effects on second messengers in adult and neonatal tissues. It stimulates phosphoinositide hydrolysis in a dose‐dependent manner in both the adult and neonate hippocampus, inhibits stimulated cAMP levels in the adult and enhances the cAMP in the neonate. It is an effective antagonist of mGluRs linked to phospholipase D (PLD) in the adult and an agonist in the neonate brain or astrocyte cultures. (S)‐3,5‐DHPG induces elevation of [Ca2+]iand regulates multiple subtypes of Ca2+channels. This agonist of group I mGluRs may modulate neurotransmitters release, reflecting the diversity of mechanisms involved. Depending on the dose, (S)‐3,5‐DHPG enhances or decreases excitatory postsynaptic potentials (EPSPs) and under appropriate conditions it can induce long‐term depression (LTD) and long‐term potentiation (LTP). Some studies suggested a therapeutic role for (S)‐3,5‐DHPG in neuronal injury, regulation of intestinal motility and secretion, learning and memory processes and in cardiovascular system.(S)‐3,5‐DHPG may be useful as a cognitive enhancing agent in memory impairment associated with ischemia or hypoxia. Recent investigations suggested possible beneficial effects of (S)‐3,5‐DHPG in Alzheimer's disease.
JL 13, An Atypical Antipsychotic: A Preclinical Review
Authors: Ellenbroek Bart A. , Liégeois Jean‐François 
Published: August 2010

ABSTRACTThe extensive pharmacological evaluation of JL 13 as an atypical antipsychotic drug has revealed a close similarity to clozapine, however with some major advantages. JL 13 was characterized as a weak D2antagonist, bothin vitroandin vivo, with a strong affinity for the D4and the 5‐HT2Areceptors. It has no affinity for the 5‐HT2Creceptor.In vivomicrodialysis experiments in rat showed that JL 13, like clozapine, preferentially increased extracellular dopamine concentrations in the prefrontal cortex compared to nucleus accumbens or striatum.Behavioral studies showed that JL 13, like clozapine, has the profile of an atypical antipsychotic. Thus, JL 13 did not antagonize apomorphine‐induced stereotypy nor did it produce catalepsy, but it antagonized apomorphine‐induced climbing in rodents. It was inactive againstd‐amphetamine‐induced stereotypy but antagonizedd‐amphetamine‐induced hyperactivity in the mouse. Likewise, in the paw test, it was more effective in prolonging hindlimb retraction time than prolonging forelimb retraction time. Like other antipsychotic drugs, JL 13 reversed the apomorphine‐ and amphetamine‐induced disruption of prepulse inhibition. In a complex temporal regulation schedule in the dog, JL 13 showed a high resemblance with clozapine without inducing sialorrhea, palpebral ptosis or any significant motor side effects. In rats and squirrel monkeys JL 13 induced a high degree of generalization (70%) to clozapine.Regarding behavioral toxicology, JL 13 did not produce dystonia or Parkinsonian symptoms in haloperidol‐sensitized monkeys. After acute administration, again like clozapine, JL 13 induced only a transient increase in circulating prolactin. Last but not the least, regarding a possible hematological toxicity, unlike clozapine, JL 13 did not present sensitivity to peroxidase‐induced oxidation. Moreover, its electrooxidation potential was close to that of loxapine and far from that of clozapine. Taking all these preclinical data into account, it appears that JL 13 is a promising atypical antipsychotic drug.
Antinociception and the New COX Inhibitors: Research Approaches and Clinical Perspectives
Authors: Herrero Juan F. , Romero‐Sandoval E. Alfonso , Gaitan Gema , Mazario Javier 
Published: August 2010

ABSTRACTNew generations of cyclooxygenase (COX) inhibitors are more potent and efficacious than their traditional parent compounds. They are also safer than the classic non‐steroidal anti‐inflammatory drugs (NSAIDs) and are starting to be used not only for low to moderate intensity pain, but also for high intensity pain. Three different strategies have been followed to improve the pharmacological profile of COX inhibitors:1. Development of COX‐2 selective inhibitors. This is based on the initial hypothesis that considered COX‐2 as the enzyme responsible for the generation of prostaglandins only in inflammation, and, therefore, uniquely responsible for inflammation, pain and fever. Initial expectations gave rise to controversial results, still under discussion. The second generation of these compounds is being developed and should contribute to clarifying both their efficacy and the specific functions of the COX enzymes.2. Modified non‐selective COX inhibitors. Molecules like nitro‐NSAIDs or tromethamine salt derivatives have been synthesized considering that both COX‐1 and COX‐2 are responsible for the synthesis of prostaglandins involved either in homeostatic functions or inflammation. Nitroaspirin, nitroparacetamol or dexketoprofen trometamol are some examples of molecules that are already showing an important clinical efficacy. The modifications performed in their structures seem to lower the unwanted side effects as well as to enhance their analgesic efficacy.3. Combined therapy of classic NSAIDs with other drugs. This strategy looks for improvements in the incidence of adverse effects or to take advantage of the synergistic enhancement of their therapeutic effects. Some of the molecules resulting from these strategies are very valuable as therapeutic agents and open a wide range of possibilities in the treatment of high intensity pain, including neuropathic pain, and opiate sparing therapy.
UFP‐101, a Peptide Antagonist Selective for the Nociceptin/Orphanin FQ Receptor
Authors: Calo Girolamo , Guerrini Remo , Rizzi Anna , Salvadori Severo , Burmeister Melissa , Kapusta Daniel R. , Lambert David G. , Regoli Domenico 
Published: August 2010

ABSTRACTNociceptin/orphanin FQ modulates various biological functions at central and peripheral levels by selectively activating a G‐protein coupled receptor named N/OFQ peptide (NOP) receptor. For extending our knowledge on the biological roles of the N/OFQ ‐ NOP receptor system the identification of selective NOP ligands, especially antagonists, is mandatory. [Nphe1, Arg14, Lys15] N/OFQ‐NH2(UFP‐101) is a novel NOP ligand that was designed by combining, in the same molecule, the [Nphe1] chemical modification which eliminates efficacy and the [Arg14, Lys15] substitution which increases ligand potency and duration of actionin vivo.In the present article, we summarize the pharmacological features of UFP‐101 as determined in a series ofin vitroandin vivoassays. Moreover, some biological actions and possible therapeutic indications of NOP ligands are discussed on the basis of results obtained with UFP‐101. Data obtained with this compound were compared with those generated using other NOP antagonists, especially J‐113397 and [Nphe1]N/OFQ(1‐13)‐NH2, receptor or peptide knockout mice and other pharmacological tools useful for blocking N/OFQ – NOP receptor signaling.The analysis of the available data demonstrates that UFP‐101 is a useful pharmacological tool for the investigation of the central and peripheral biological functions regulated by the N/OFQ – NOP receptor system and for defining the therapeutic potential of NOP receptor ligands
Neuroprotection by Rasagiline: A New Therapeutic Approach to Parkinson's Disease?
Authors: Blandini Fabio 
Published: August 2010

ABSTRACTNeuronal death in Parkinson's disease (PD) may originate from the reciprocal interactions of a restricted number of conditions, such as mitochondrial defects, oxidative stress and protein mishandling, which would favor a state of apoptotic cell death in the nigrostriatal pathway. The search for pharmacological treatments able to counteract the nigrostriatal degeneration, possibly by interfering with these phenomena, has recently raised considerable interest in rasagiline [R(+)‐N‐propargyl‐1‐aminoindan], a potent, selective, and irreversible inhibitor of monoamine oxidase B (MAO‐B). Rasagiline, like selegiline, is a propargylamine, but is ∼10 times more potent. Unlike selegiline, rasagiline is not metabolized to amphetamine and/or methamphetamine and is devoid of sympathomimetic activity. Numerous experimental studies, conducted both in vitro and in vivo, have shown that rasagiline possesses significant protective properties on neuronal populations. The pro‐survival effects of the drug appear to be linked to its propargyl moiety, rather than to the inhibitory effect on MAO‐B. Rasagiline's major metabolite, aminoindan — which possesses intrinsic neuroprotective activity — may also contribute to the beneficial effects of the parent compound.Rasagiline has been recently evaluated in early PD patients, with results that are consistent with slowing the progression of the disease. Therefore, the neuroprotective activity shown by the drug under experimental conditions may be reflected in the clinic, thus providing new perspectives for the treatment of PD.
Trade Liberalization and Peripheral Postindustrialization in the Caribbean
Authors: Pantojas-García Emilio 
Published: August 2010

AbstractIn the 1990s, trade liberalization eroded the competitiveness of Caribbean economies as manufacturing export platforms. Proposed new economic strategies favored a shift from vertically integrated, transnationally based segment manufacturing to segments of knowledge-intensive industries and services. This strategy, however, reproduces the economic asymmetries associated with the core-periphery relation (low wages, value-added rates). Postindustrial technologies and economic strategies provide the opportunity to formulate alternative policies to overcome the shortcomings of peripheral postindustrialization and foster sustainable postindustrial development.
Explicit Narcotization: U.S. Policy Toward Colombia During the Samper Administration
Authors: Crandall Russell 
Published: August 2010

AbstractSuspecting that his electoral campaign had received contributions from the Cali drug cartel, the U.S. government considered Colombian president Ernesto Samper (1994–98) an enemy in the drug war. U.S. antidrug policy accordingly targeted not just illicit crop cultivation, traffickers, and money laundering but also the democratically elected president himself. In many ways, U.S. policy became obsessed with bringing down Samper, an “explicit narcotization” that had severe consequences for the two countries' relationship. This case study analyzes the often complex interactions between dominant and subordinate states, especially when the dominant state's involvement in the subordinate state is driven by domestic political concerns.
The New Federalism in Mexico and Foreign Economic Policy: An Alternative Two-Level Game Analysis of the Metalclad Case
Authors: Tamayo Arturo Borja 
Published: August 2010

AbstractThis article examines, through a two-level game model, the case of the first investment dispute under NAFTA between a private U.S. firm and the Mexican government. It argues that the clue to understanding why the Mexican president could not cooperate with the U.S. president lies in Mexico's domestic “ratification” process. The analysis yields two theoretical propositions. First, federalism represents an important variable in explaining foreign economic policy. Second, two-level game logic should not be applied only to formal international negotiation situations; instead, by specifying the dependent variable as cooperation or noncooperation, these models connecting domestic and international politics can be productively applied to study foreign economic policy.
State Developmentalism Without a Developmental State: The Public Foundations of the “Free Market Miracle” in Chile
Authors: Kurtz Marcus 
Published: August 2010

AbstractIf export orientation is a goal in a sustainable development strategy, this study argues that public interventions at the sectoral level in a variety of markets can produce economic reorientation that pursues international comparative advantage faster and at lower cost than free market forces can. Pervasive failures in information, credit, input, distribution, and insurance markets can render strictly market-based adjustment both slow and costly. Although Chile's export boom and high growth rates have been associated with its free market economic policies, this article, based on a comparison of the fruit, fish, and forestry sectors, contends that new forms of public intervention were crucial catalysts in shaping a sustained export response.
Strong Societies, Weak Parties: Regime Change in Cuba and Venezuela in the 1950s and Today
Authors: Corrales Javier 
Published: August 2010

AbstractThe literature on the origins of democratic institutions is split between bottom-up and top-down approaches. The former emphasize societal factors that press for democracy; the latter, rules and institutions that shape elites' incentives. Can these approaches be reconciled? This article proposes competitive political parties, more so than degrees of modernization and associationalism, as the link between the two. Competitive political parties enhance society's bargaining power with the state and show dominant elites that liberalization is in their best interest; the parties are thus effective conduits of democracy. In the context of party deficit, the prospects for democratization or redemocratization are slim. This is illustrated by comparing Cuba and Venezuela in the 1950s and 1990s.
Can International Boycotts Transform Political Systems? The Cases of Cuba and South Africa
Authors: Schwartzman Kathleen C. 
Published: August 2010

AbstractThe economic embargo against Cuba has been widely promoted as a way to hasten the end of the Castro regime. Historically, however, the connection between embargoes and regime change is mediated by a complex of political, social, and economic conditions. Labormarket bottlenecks and domestic elite opposition, decisive factors in the South African case, are absent from that of Cuba. This study uses the factors derived from an analysis of South Africa to compare the Cuban case and concludes that the embargo against Cuba cannot have its intended results.
The Elusive Goal in Democratic Chile: Reforming the Pinochet Labor Legislation
Authors: Frank Volker 
Published: August 2010

AbstractDespite major attempts by the three governments of the post-Pinochet era, the promised reform of the labor legislation inherited from the military regime remains essentially incomplete. This study attempts to explain why, and addresses some of the consequences of this delay for Chilean organized labor, examining particularly the variables of consensus politics and employer concessions.
Social Control in Cuba
Authors: Aguirre Benigno E. 
Published: August 2010

AbstractWhy has the Cuban government been so successful in its system of social control, and why might that system's effectiveness now be on the wane? This study argues that Cuba combines formal and informal systems of control that simultaneously emphasize openness and rigidity. The formal system is geared to block all antihegemonic acts, particularly those that, if left unchecked, could become symbolic acts encouraging similar behavior that the authorities deem undesirable. The system favors reactive rather than proactive approaches, as exemplified by the rapid action brigades. Noninstitutionalized collective behavior is also taking place, as is the emergence of civil society.
Community Participation, the Environment, and Democracy: Brazil in Comparative Perspective
Authors: Jacobs Jamie Elizabeth 
Published: August 2010

AbstractGrassroots environmental activism among Latin America's poor has altered the debate over environmental policy, social welfare, and citizenship. Yet the question remains whether this social mobilization of the poor is part of a larger trend toward broader environmental concerns and democratic political participation, or a shortlived movement susceptible to the same pressures that have dissolved community mobilization in the past. This article compares Brazil with other Latin American and European countries in surveys of environmental awareness, concerns, and reported behavior. It finds that Brazilians residing in the urban periphery link their own local environmental concerns to more global considerations, and that concern for and activism on environmental issues is positively related to wider community involvement.
From Antagonistic Autonomy to Relational Autonomy: A Theoretical Reflection from the Southern Cone
Authors: Russell Roberto , Tokatlian Juan Gabriel 
Published: August 2010

AbstractThe concept of autonomy has acquired a plurality of meanings in international relations; this article analyzes the distinct uses given to this term in Latin America and its relationship to theoretical contributions from outside the region. The authors propose a far-reaching reconceptualization of autonomy appropriate to Latin America's new circumstances in the global context. They argue that these new circumstances favor the shift from autonomy as traditionally defined to what they call relational autonomy, a construct based on contributions from classical political theory, political sociology, gender studies, social and philosophical psychology, and the theory of complex thought.
Thinking outside the (Ballot) Box: Informal Electoral Institutions and Mexico's Political Opening
Authors: Eisenstadt Todd A. 
Published: August 2010

AbstractThis article studies the development of informal bargaining tables to mitigate postelectoral conflicts in some 15 percent of Mexico's local elections between 1989 and 2000, even as formally autonomous electoral commissions and courts were being constituted. By documenting the dual institutions that resulted, the study qualifies theories of institutional design that take actor consent for granted. It argues that in the Mexican case and perhaps others, elections, particularly subnational elections, are focal points for informal bargaining over rules that are the true motors of protracted transitions. It finds electoral institutions to be critical to democratization, but for reasons beyond those given by most institutionalists.
A Preferential Option for the Spirit: The Catholic Charismatic Renewal in Latin America's New Religious Economy
Authors: Chesnut R. Andrew 
Published: August 2010

AbstractThe Catholic Charismatic Renewal (CCR), the Latin American church's largest and most dynamic lay movement, demands scholarly attention for its extraordinary appeal among Catholic laity and its unanimous approval by national episcopacies. If the church is finally using mass media and other Protestant techniques for evangelization, it is because of the Charismatics, whose missionary zeal rivals that of their chief competitors, the Pentecostals. This study uses the tools of religious economy to analyze the reasons for the Renewal's rapid growth and acceptance. In attempting to explicate the CCR's success, the study also examines the major ecclesial trends during the movement's three decades in Latin America.
The Reelection Debate in Latin America
Authors: Carey John M. 
Published: August 2010

AbstractThe debate over presidential reelection reappeared in Latin America in the last decade, and promises to continue in the years ahead. Arguments in favor contend that the possibility of immediate reelection increases politicians' responsiveness to citizen demands and allows voters the freedom to retain popular incumbents. Arguments against emphasize the danger of abuse of power by incumbents who seek to prolong their tenure. This article illustrates the parallels between these arguments and those made historically regarding the issue. It also suggests that the means by which provisions to allow reelection are adopted can provide valuable signals of their consequences.