title: Behavioral effects of the imidazoline I(2) receptor ligand BU99006 in rats.
abstract: The imidazoline I2 receptor ligand BU99006 binds to and attenuates effects mediated by I2 receptors in vitro, although its effects in vivo have not been studied previously. This study examined the effects of BU99006 in two behavioral assays in rats: hypothermia and 2-BFI discrimination. BU99006 (3.2-15 mg/kg, intraperitoneally) produced a dose-dependent hypothermic effect (rectal temperature), which was antagonized by the I2 receptor antagonist idazoxan. BU99006 (3.2 or 10 mg/kg administered 10 min or 2 h before the session, respectively) did not significantly alter hypothermia produced by the I2 receptor agonist 2-BFI (10 mg/kg). In rats discriminating 5.6 mg/kg 2-BFI, BU99006 (1.78-17.8 mg/kg, intraperitoneally) produced 40 and 82% responding on the 2-BFI-associated lever when it was administered immediately or 2 h before the test sessions, respectively. BU99006 enhanced the discriminative stimulus and rate-suppressing effects of 2-BFI. Collectively, these data suggest that BU99006 is an imidazoline I2 receptor agonist with no evidence of I2 receptor antagonism in rats.
authors: aDepartment of Physiology, School of Basic Medical Sciences, Wuhan University, Hubei, People's Republic of China bDepartment of Pharmacology and Toxicology, School of Medicine and Biomedical Sciences, University at Buffalo, State University of New York, Buffalo, New York cResearch Triangle Institute, Research Triangle Park, North Carolina, USA.
authors: Yanyan
authors: Y
authors: Qiu
authors: David A
authors: DA
authors: Thorn
authors: Yanan
authors: Y
authors: Zhang
authors: Xiaohua
authors: X
authors: He
authors: Jun-Xu
authors: JX
authors: Li
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000494:pharmacology*; D001831:Body Temperature / Q000187:drug effects*; D002491:Central Nervous System Agents / Q000494:pharmacology*; D004192:Discrimination, Psychological / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D007035:Hypothermia / Q000139:chemically induced*; D019329:Idazoxan / Q000494:pharmacology; D007093:Imidazoles / Q000494:pharmacology*; D054755:Imidazoline Receptors / Q000819:agonists* / Q000037:antagonists & inhibitors; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C468012:BU 99006; D001572:Benzofurans; D002491:Central Nervous System Agents; D007093:Imidazoles; D054755:Imidazoline Receptors; C103723:2-(2-benzofuranyl)-2-imidazoline; D019329:Idazoxan