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CL-218,872



CL-218,872
Systematic (IUPAC) name
3-methyl-6-[3-(trifluoromethyl)phenyl]-[1,2,4]triazolo[3,4-f]pyridazine
Identifiers
CAS number 66548-69-4
ATC code  ?
PubChem 107950
Chemical data
Formula C13H9F3N4 
Mol. mass 278.233 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

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

  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. 1994 Jul 8;37(14):2153-60.
  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 and Medicinal Chemistry. 1994 Aug;2(8):773-9.
  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. 1995 Nov 30;291(3):301-9.
  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. 1996 Nov 1;271(44):27902-11.
  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. 1999 Mar;20(3):255-62.
  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 (Berlin). 2003 Jan;165(3):209-15.
  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. 2003 Dec;6(6):379-87.
  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. Journal of Pharmacology and Experimental Therapeutics. 2006 Mar;316(3):1291-9.
v • d • e
Psycholeptics: hypnotics and sedatives (N05C)
BarbituratesPentobarbital - Amobarbital - Butobarbital - Barbital - Aprobarbital - Secobarbital - Talbutal - Vinylbital - Vinbarbital - Cyclobarbital - Heptabarbital - Reposal - Methohexital - Hexobarbital - Thiopental - Ethallobarbital - Allobarbital - Proxibarbal - Phenobarbital
AldehydesAcetylglycinamide chloral hydrate - Chloral hydrate - Chloralodol - Dichloralphenazone - Paraldehyde - Petrichloral
BenzodiazepineBrotizolam - Cinolazepam - Doxefazepam - Estazolam - Flunitrazepam - Flurazepam - Loprazolam - Lorazepam - Lormetazepam - Nitrazepam - Nimetazepam - Midazolam - Quazepam - Temazepam - Triazolam
PiperidinedioneGlutethimide - Methyprylon - Pyrithyldione
QuinazolinoneAfloqualone - Cloroqualone - Diproqualone - Etaqualone - Mebroqualone - Mecloqualone - Methaqualone - Methylmethaqualone
NonbenzodiazepineCL-218,872 - Eszopiclone - Indiplon - Necopidem - Pazinaclone - Saripidem - Suproclone - Suriclone - SX-3228 - Zaleplon - Zolpidem - Zopiclone
Melatonin receptorAgomelatine - Melatonin - Ramelteon
GHB TypeGABOB - GHB - GBL - 1,4-Butanediol
OtherApronal - Bromides - Bromisoval - Carbromal - Clomethiazole - Dexmedetomidine - Embutramide - Ethchlorvynol - Ethinamate - Hexapropymate - Methylpentynol - Niaprazine - Propiomazine - Scopolamine - Sulfonmethane - Trichloroethanol - Triclofos - Valerian - Valnoctamide
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "CL-218,872". A list of authors is available in Wikipedia.
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