CL-218,872

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IUPAC_name = 3-methyl-6- [3-(trifluoromethyl)phenyl] - [1,2,4] triazolo [3,4-f] pyridazine

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CAS_number = 66548-69-4
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PubChem = 107950
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C=13|H=9|F=3|N=4
molecular_weight = 278.233 g/mol
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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 [b] -heteroannulated pyridazine derivatives--II. Structure-activity relationships in the 6-aryltriazolo- [4,3-b] 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 GABA_A 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 [3H] 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.]

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