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NCS-382

Introduction

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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