NCS-382 explained

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 the genetic metabolic disorder succinic semialdehyde dehydrogenase deficiency (SSADHD), but has never been developed for clinical use.[6]

Notes and 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 . 10 . 3 . 243–260 . 15492774 . 10.1111/j.1527-3458.2004.tb00025.x . 6741708 .
  2. Ticku MK, Mehta AK . Characterization and pharmacology of the GHB receptor . Annals of the New York Academy of Sciences . 1139 . 1. 374–385 . October 2008 . 18991884 . 10.1196/annals.1432.048 . 2008NYASA1139..374T . 37091049 .
  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 . Nov 1990 . 255 . 2 . 657–63. 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 . Oct 1991 . 203 . 3 . 393–7. 1773824 . 10.1016/0014-2999(91)90896-X .
  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 & Behavior . Sep 1995 . 58 . 3 . 587–590 . 8587968 . 10.1016/0031-9384(95)00086-X . 45842160 .
  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 . Jul 2002 . 302 . 1 . 180–187 . 12065715 . 10.1124/jpet.302.1.180 . 24503217 .

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