Examining the Effects of (α4)3(β2)2 Nicotinic Acetylcholine Receptor-Selective Positive Allosteric Modulator on Acute Thermal Nociception in Rats

Autor:	Farah Deba, Kara Ramos, Matthew Vannoy, Kemburli Munoz, Lois S. Akinola, M. Imad Damaj, Ayman K. Hamouda
Jazyk:	angličtina
Rok vydání:	2020
Předmět:	nicotinic acetylcholine receptors (nAChRs) positive allosteric modulators (PAMs) desformylflustrabromine (dFBr) CMPI acute thermal nociception hot plate Organic chemistry QD241-441
Zdroj:	Molecules, Vol 25, Iss 12, p 2923 (2020)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules25122923
Popis:	Neuronal nicotinic acetylcholine receptor (nAChR)-based therapeutics are sought as a potential alternative strategy to opioids for pain management. In this study, we examine the antinociceptive effects of 3-(2-chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole (CMPI), a novel positive allosteric modulator (PAM), with preferential selectivity to the low agonist sensitivity (α4)3(β2)2 nAChR and desformylflustrabromine (dFBr), a PAM for α4-containing nAChRs. We used hot plate and tail flick tests to measure the effect of dFBr and CMPI on the latency to acute thermal nociceptive responses in rats. Intraperitoneal injection of dFBr, but not CMPI, dose-dependently increased latency in the hot plate test. In the tail flick test, the effect achieved at the highest dFBr or CMPI dose tested was only
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/b51df15f92344ed789de3fb3583a5d8a Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.