Detail of "130477-52-0"

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Behavioral profile of L-655,708, a selective ligand for the benzodiazepine site of GABA-A receptors which contain the a5 subunit, in social encounters between male mice

Behavioral profile of L-655,708, a selective ligand for the benzodiazepine site of GABA-A receptors which contain the a5 subunit, in social encounters between male mice. Navarro, Jose Francisco; Buron, Estrella; Martin-Lopez, Mercedes ( Department of Psychobiology, Faculty of Psychology, University of Malaga, Spain). Aggressive Behavior, 30(4), 319-325 (English) 2004 Wiley-Liss, Inc. CODEN: AGBEDU. ISSN: 0096-140X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 GABA-A receptor is a transmembrane hetero-oligomeric protein which consists of five subunits, the combination of which confers unique pharmacol. properties to the receptor.There are some reagents like 130477-52-0 is used in this study. It is well-known that the GABAergic system is involved in the modulation of aggression. However, the role of a5/GABA-A receptors has not been explored. In this study, we examd. the effect of L-655,708 (0.625-5 mg/kg), a selective ligand for the benzodiazepine site of GABA-A receptors which contain the a5 subunit, on agonistic behavior elicited by isolation in male mice. Individually housed mice were exposed to an anosmic "std. opponent" 30 min after drug administration, and the encounters were videotaped and evaluated using an ethol. based anal. L-655,708 (5 mg/kg) exhibited an ethopharmacol. profile characterized by a marked redn. of the time spent in offensive behavior (threat and attack) without affecting immobility, accompanied by a significant increase of avoidance/flee and nonsocial exploration behaviors, suggesting that the antiaggressive effect of the drug is unselective. Overall, this behavioral profile might indicate the existence of an anxiogenic-like activity of L-655,708 in mice. .

[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the a5 subunit

[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the a5 subunit. Quirk, K.; Blurton, P.; Fletcher, S.; Leeson, P.; Tang, F.; Mellilo, D.; Ragan, C. I.; Mckernan, R. M. (Department of Biochemistry and Merck Sharp and Dohme Research Laboratories, Essex CM20 2QR, UK). Neuropharmacology, 35(9/10), 1331-1335 (English) 1996 Elsevier. CODEN: NEPHBW. ISSN: 0028-3908. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 8, 9 A compd. (L-655,708) has been identified which has at least 50-fold selectivity for the benzodiazepine site on GABAA receptors contg. an a5 subunit over those contg. an a1, a2, a3 or a6 subunit in combination with b3 and g2. The compd. was radiolabeled with tritium and investigated as a novel radioligand which recognizes the benzodiazepine site of GABAA receptors which contain the a5 subunit. [3H]L-655,708 labels one saturable and specific population of binding sites in rat hippocampus with a Kd of 2.4 nM and a Bmax of 256 fmol/mg protein. The pharmacol. 130477-52-0 and 187622-71-5 which are cas registry numbers of substances are two of reagents here. of the binding site labeled was consistent with that of receptors present in cells transfected with a5, b2 and g2 and with receptors immunopptd. from rat brain with an a5-selective antiserum. It is concluded that [3H]L-655,708 is the first radioligand to date which is selective for any BZ2 subtype of the GABAA receptor and should provide a valuable tool for elucidating the structure and function of the a5-contg. GABAA receptor subtype. .