NCS-382

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NCS-382 is a moderately selective antagonist for the GHB receptor.[1] It blocks the effects of GHB in animals and has both anti-sedative and anticonvulsant effects.[2][3][4] 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.[5]


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. 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
  3. 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
  4. 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
  5. 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

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