N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists

Autor:	Yoshifumi Togo, Masakazu Fujio, Yasunori Morio, Yasuhiro Matsumoto, Takanobu Kuroita, Hideo Tomozane, Jiro Katayama
Rok vydání:	2000
Předmět:	Agonist Pyrrolidines medicine.drug_class Stereochemistry Oxamide Clinical Biochemistry Pharmaceutical Science Carboxamide In Vitro Techniques Biochemistry Chemical synthesis Binding Competitive chemistry.chemical_compound Drug Discovery polycyclic compounds medicine Animals heterocyclic compounds Receptor Serotonin 5-HT2A Receptor Molecular Biology Neurons Chemistry Receptors Dopamine D2 organic chemicals musculoskeletal neural and ocular physiology Organic Chemistry Amides Rats Serotonin Receptor Agonists nervous system Receptors Serotonin Molecular Medicine 5-HT1A receptor Raphe Nuclei Enantiomer Selectivity Receptors Serotonin 5-HT1
Zdroj:	Bioorganicmedicinal chemistry letters. 10(5)
ISSN:	0960-894X
Popis:	A series of benzamides was synthesized as selective agonists for the 5-HT1A receptor. It was found that (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarb oxamide(7-(S)) has potent and selective agonistic activity for the 5-HT1A receptor (5-HT1A; Ki 0.49 nmol/L, D2; IC50 = >1000 nmol/L, 5-HT2; Ki = 240 nmol/L).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::836bbebae019b0c9d13480af593b5b55 https://pubmed.ncbi.nlm.nih.gov/10743959 Zobrazit plný text záznamu Full Text from ScienceDirect