CL-218,872 explained

CL-218,872 is a sedative and hypnotic drug used in scientific research.^{[1] [2]} 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.^{[3] [4] [5]} 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.^{[6] [7] [8]}

Notes and References

1. 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 . 37 . 14 . 2153–60 . July 1994 . 8035421 . 10.1021/jm00040a006 .
2. 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 & Medicinal Chemistry . 2 . 8 . 773–9 . August 1994 . 7894970 . 10.1016/s0968-0896(00)82176-8 .
3. 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 . 291 . 3 . 301–9 . November 1995 . 8719414 . 10.1016/0922-4106(95)90070-5 .
4. 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 . November 1996 . 271 . 44 . 27902–11 . 10.1074/jbc.271.44.27902 . 8910390 . free .
5. 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 . 20 . 3 . 255–62 . March 1999 . 10063485 . 10.1016/S0893-133X(98)00052-9 . free .
6. 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 . 165 . 3 . 209–15 . January 2003 . 12420154 . 10.1007/s00213-002-1275-z . 37632215 .
7. 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 . 6 . 6 . 379–87 . December 2003 . 14744042 . 10.1080/10284150310001624200 . 26974393 .
8. 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 . The Journal of Pharmacology and Experimental Therapeutics . 316 . 3 . 1291–9 . March 2006 . 16339395 . 10.1124/jpet.105.094003 . 21913400 .