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CL-218,872
CL-218,872 is a sedative and hypnotic drug used in scientific research.〔Moreau S, Coudert P, Rubat C, Gardette D, Vallee-Goyet D, Couquelet J, Bastide P, Tronche P. Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. ''Journal of Medicinal Chemistry''. 1994 Jul 8;37(14):2153-60.〕〔Karolak-Wojciechowska J, Lange J, Kwiatkowski W, Gniewosz M, Plenkiewicz J. Bicyclic ()-heteroannulated pyridazine derivatives--II. Structure-activity relationships in the 6-aryltriazolo-()pyridazine ligands of the benzodiazepine receptor. ''Bioorganic and Medicinal Chemistry''. 1994 Aug;2(8):773-9.〕 It has similar effects to sedative-hypnotic benzodiazepine drugs such as triazolam, but is structurally distinct and so is classed as a nonbenzodiazepine hypnotic.
CL-218,872 is a GABAA partial agonist which is selective for the α1 subtype.〔Hadingham KL, Wafford KA, Thompson SA, Palmer KJ, Whiting PJ. Expression and pharmacology of human GABAA receptors containing gamma 3 subunits. ''European Journal of Pharmacology''. 1995 Nov 30;291(3):301-9.〕〔Araujo F, Tan S, Ruano D, Schoemaker H, Benavides J, Vitorica J. Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits. ''Journal of Biological Chemistry''. 1996 Nov 1;271(44):27902-11.〕〔Atack JR, Smith AJ, Emms F, McKernan RM. Regional differences in the inhibition of mouse in vivo ()Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors. ''Neuropsychopharmacology''. 1999 Mar;20(3):255-62.〕 It has a range of effects including sedative, hypnotic, anxiolytic, anticonvulsant and amnestic actions, however the most prominent actions are sedation and amnesia, and CL-218,872 produces effects very similar to those of the hypnotic imidazopyridine derivative zolpidem in animal studies.〔Rowlett JK, Spealman RD, Lelas S, Cook JM, Yin W. Discriminative stimulus effects of zolpidem in squirrel monkeys: role of GABA(A)/alpha1 receptors. ''Psychopharmacology (Berlin)''. 2003 Jan;165(3):209-15.〕〔Tonkiss J, Shultz PL, Bonnie KE, Hudson JL, Duran P, Galler JR. Spatial learning deficits induced by muscimol and CL218,872: lack of effect of prenatal malnutrition. ''Nutritional Neuroscience''. 2003 Dec;6(6):379-87.〕〔Mirza NR, Rodgers RJ, Mathiasen LS. Comparative cue generalization profiles of L-838, 417, SL651498, zolpidem, CL218,872, ocinaplon, bretazenil, zopiclone, and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination. ''Journal of Pharmacology and Experimental Therapeutics''. 2006 Mar;316(3):1291-9.〕
== References ==
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