NCS-382

NCS-382
NCS-382
IUPAC name
(2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene ethanoic acid
Identifiers
CAS number 131733-92-1
PubChem 23714994
MeSH NCS-382
Jmol-3D images Image 1
Properties
Molecular formula C13H14O3
Molar mass 218.248
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Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

NCS-382 is a moderately selective antagonist for the GHB receptor.[1][2] It blocks the effects of GHB in animals and has both anti-sedative and anticonvulsant effects.[3][4][5] It has been proposed as a treatment for GHB overdose in humans, as well as for the endogenous metabolic disorder succinic semialdehyde dehydrogenase deficiency, but has never been developed for clinical use.[6]


References

  1. ^ Castelli MP, Pibiri F, Carboni G, Piras AP. A review of pharmacology of NCS-382, a putative antagonist of gamma-hydroxybutyric acid (GHB) receptor. CNS Drug Reviews. 2004 Fall;10(3):243-60. PMID 15492774
  2. ^ Ticku MK, Mehta AK (October 2008). "Characterization and pharmacology of the GHB receptor". Annals of the New York Academy of Sciences 1139: 374–85. doi:10.1196/annals.1432.048. PMID 18991884. 
  3. ^ Maitre M, Hechler V, Vayer P, Gobaille S, Cash CD, Schmitt M, Bourguignon JJ. A specific gamma-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties. Journal of Pharmacology and Experimental Therapeutics. 1990 Nov;255(2):657-63. PMID 2173754
  4. ^ Schmidt C, Gobaille S, Hechler V, Schmitt M, Bourguignon JJ, Maitre M. Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist. European Journal of Pharmacology. 1991 Oct 22;203(3):393-7. PMID 1773824
  5. ^ Colombo G, Agabio R, Bourguignon J, Fadda F, Lobina C, Maitre M, Reali R, Schmitt M, Gessa GL. Blockade of the discriminative stimulus effects of gamma-hydroxybutyric acid (GHB) by the GHB receptor antagonist NCS-382. Physiology and Behaviour. 1995 Sep;58(3):587-90. PMID 8587968
  6. ^ Gupta M, Greven R, Jansen EE, Jakobs C, Hogema BM, Froestl W, Snead OC, Bartels H, Grompe M, Gibson KM. Therapeutic intervention in mice deficient for succinate semialdehyde dehydrogenase (gamma-hydroxybutyric aciduria). Journal of Pharmacology and Experimental Therapeutics. 2002 Jul;302(1):180-7. PMID 12065715


v · d · eGHBergics
Receptor
ligands
1,4-BD • 4-Methyl-GHB • GABOB • GBL • GHB • GHV • GVL • NCS-356 • NCS-435 • T-HCA • UMB66 • UMB68 • UMB72 • UMB86; Benzamides: Amisulpride • Sulpiride • Sultopride
NCS-382


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