Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist

Autor:	Sanner Mark Allen, Desai Kishor A, Celeste Johnson, Jae S. Lee, Judith L. Collins, Audrey R. Dunaiskis, W. Stephen Faraci, Cecilia C. Di Prete, Angela Trozzi, Thomas Allen Chappie, Patricia A. Seymour, Jean Morrone, David B. Duignan, Stevin H. Zorn, Mark J. Majchrzak, Jackson Elisa Rose, Fliri Anton F J
Rok vydání:	1999
Předmět:	Pyrazine Apomorphine medicine.drug_class Clinical Biochemistry Pharmaceutical Science Pharmacology Motor Activity Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship In vivo Dopamine Drug Discovery medicine Animals Receptor Molecular Biology Molecular Structure Chemistry Organic Chemistry Receptors Dopamine D4 Antagonist Receptor antagonist In vitro Rats Dopamine D2 Receptor Antagonists Pyrimidines Drug Design Pyrazines Molecular Medicine Dopamine Antagonists Haloperidol Indicators and Reagents medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 8(7)
ISSN:	0960-894X
Popis:	A series of novel, potent and selective pyrido[1,2-a]pyrazine dopamine D4 receptor antagonists are reported including CP-293,019 (D4 Ki = 3.4 nM, D2 Ki > 3,310 nM), which also inhibits apomorphine-induced hyperlocomotion in rats after oral dosing.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e87bcf9121789661fcccc9f11a1f8abb https://pubmed.ncbi.nlm.nih.gov/9871530 Zobrazit plný text záznamu Full Text from ScienceDirect