Development of a New Polymeric Nanocarrier Dedicated to Controlled Clozapine Delivery at the Dopamine D2-Serotonin 5-HT1A Heteromers

Partial Dopamine D2/Serotonin 5-HT1A Receptor Agonists as New Therapeutic Agents

The therapeutic efficacy of current antipsychotic or antidepressant agents still present important drawbacks such as delayed onset of action and a high percentage of non-responders. Despite significant advancements in the development of new drugs with more acceptable side-effect profiles, patients with schizophrenia or major depression experience substantial disability and burden of disease. Th...

Bifeprunox: a novel antipsychotic agent with partial agonist properties at dopamine D2 and serotonin 5-HT1A receptors

Most second-generation, atypical, dopamine (DA) D2/5-HT2 blocking antipsychotics still induce extrapyramidal side effects (EPS) in higher doses. Weight gain and metabolic disturbances are also a problem, and negative and cognitive symptoms have not been sufficiently addressed. The current brain DA mesolimbic hyperactive/mesocortical hypoactive hypothesis of schizophrenia suggests that DA D2/5-H...

Mucoadhesion : a New Polymeric Controlled Drug Delivery

Since last three decades delivery of the desired drug as muocoadhesive drug delivery systems has been subject of interest. Mucoadhesion involving a polymeric drug delivery system is a complex phenomenon that includes theory of diffusion, wetting, adsorption, fracture and interpenetration of polymer chains amongst various other processes. Various polymer-based properties such as the degree of cr...

Estrogen treatment blocks 8-OH-DPAT- and apomorphine-induced disruptions of prepulse inhibition: Involvement of dopamine D1 or D2, serotonin 5-HT1A, 5-HT2A or 5-HT7 receptors*

Clozapine increases dopamine release in prefrontal cortex by 5-HT1A receptor activation.

Clozapine (1-10 mg/kg s.c.) produces a selective increase in dopamine release in rat prefrontal cortex which is, in large part (approximately 50%), mediated via activation of 5-HT1A receptors. Clozapine is a moderately potent, partial 5-HT1A receptor agonist and activation of 5-HT1A receptors may contribute to its efficacy against negative symptoms and reduced extrapyramidal side effect liabili...