Stimulus properties of arylpiperazines: NAN-190, a potential 5-HT1A serotonin antagonist

Autor:	Milt Titeler, J. L. Herndon, Richard A. Glennon, M E Pierson, Robert A. Lyon, B. Misenheimer, Noreen Naiman
Rok vydání:	1989
Předmět:	Agonist medicine.drug_class Chemistry musculoskeletal neural and ocular physiology Antagonist Stimulus (physiology) Pharmacology nervous system Radioligand binding Drug Discovery polycyclic compounds medicine heterocyclic compounds Serotonin Drug discrimination 5-HT receptor NAN-190
Zdroj:	Drug Development Research. 16:335-343
ISSN:	1098-2299 0272-4391
DOI:	10.1002/ddr.430160227
Popis:	Arylpiperazines have been demonstrated to bind both at 5-HT1A and 5-HT1B serotonin receptors. In an attempt to design novel 5-HT1A agonists and antagonists, based on an arylpiperazine nucleus, we investigated the stimulus properties of a series of such agents (in rats trained to discriminate 0.5 mg/kg of the 5-HT1B agent TFMPP from saline) to determine what structural features were important for 5-HT1B activity. This done, we modified these agents to eliminate those features and, at the same time, incorporated structural features that appeared important for 5-HT1A affinity. The resulting agents displayed high affinity for 5-HT1A sites. One agent in particular, NAN-190, neither mimicked nor antagonized the TFMPP stimulus, but was capable of antagonizing the stimulus produced by the 5-HT1A agonist 8-OH DPAT (0.2 mg/kg). These preliminary results suggest that NAN-190 may be a potential 5-HT1A antagonist.
Databáze:	OpenAIRE
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