Selective dopamine D4 receptor antagonists

Autor:	Sanner Mark Allen
Rok vydání:	1998
Předmět:	Pharmacology business.industry medicine.drug_class medicine.medical_treatment Atypical antipsychotic General Medicine medicine.disease Schizophrenia Dopamine Dopamine receptor D2 Drug Discovery Medicine Potency Receptor business Antipsychotic Clozapine medicine.drug
Zdroj:	Expert Opinion on Therapeutic Patents. 8:383-393
ISSN:	1744-7674 1354-3776
Popis:	The discovery that the atypical antipsychotic clozapine has higher affinity for the dopamine D4 receptor relative to the D2 receptor touched off a search for more potent, highly selective D4 antagonists as a new class of antipsychotics. Many compounds achieving high potency and selectivity are now available including L-745,870 (Merck), NGD 94-1 (Neurogen), PNU-101,387 (Pharmacia & Upjohn), CP-293,019 (Pfizer), and PD-172,938 (Warner-Lambert). Unfortunately, L-745,870 did not improve psychotic symptoms in a Phase II clinical trial, causing many researchers to question the role of the D4 receptor in the aetiology of schizophrenia. Recent findings with new biological models and D4 selective agonists may help clarify D4 receptor physiology.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::7a32587b2f0f7c7efdf4064b959111dd https://doi.org/10.1517/13543776.8.4.383 Zobrazit plný text záznamu