Chemistry:CL-218,872
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Short description: Chemical compound
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| Formula | C13H9F3N4 |
| Molar mass | 278.238 g·mol−1 |
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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 GABAA 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]
References
- ↑ "Synthesis and anticonvulsant properties of new benzylpyridazine derivatives". Journal of Medicinal Chemistry 37 (14): 2153–60. July 1994. doi:10.1021/jm00040a006. PMID 8035421.
- ↑ "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. doi:10.1016/s0968-0896(00)82176-8. PMID 7894970.
- ↑ "Expression and pharmacology of human GABAA receptors containing gamma 3 subunits". European Journal of Pharmacology 291 (3): 301–9. November 1995. doi:10.1016/0922-4106(95)90070-5. PMID 8719414.
- ↑ "Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits.". Journal of Biological Chemistry 271 (44): 27902–11. November 1996. doi:10.1074/jbc.271.44.27902. PMID 8910390.
- ↑ "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. doi:10.1016/S0893-133X(98)00052-9. PMID 10063485.
- ↑ "Discriminative stimulus effects of zolpidem in squirrel monkeys: role of GABA(A)/alpha1 receptors". Psychopharmacology 165 (3): 209–15. January 2003. doi:10.1007/s00213-002-1275-z. PMID 12420154.
- ↑ "Spatial learning deficits induced by muscimol and CL218,872: lack of effect of prenatal malnutrition". Nutritional Neuroscience 6 (6): 379–87. December 2003. doi:10.1080/10284150310001624200. PMID 14744042.
- ↑ "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. doi:10.1124/jpet.105.094003. PMID 16339395.
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