NCS-382

NCS-382
NCS-382
NCS-382.png
이름
IUPAC 이름
(2E)-(5-히드록시-5,7,8,9-테트라히드로-6H-벤조[a][7]안눌렌-6-일리덴에탄산
식별자
3D 모델(JSmol)
켐스파이더
메쉬 NCS-382
유니
  • InChI=1S/C13H14O3/c14-12(15)8-10-6-3-5-4-1-2-7-11(9)13(10)16/h1-2,4,7-8, ☒N13,16H,3,5-6H2,(H,14-15)10
    키: UADPGHINQMWEAG-CSKARUKUSA-N ☒N
  • InChI=1/C13H14O3/c14-12(15)8-6-3-5-5-4-1-2-7-11(9)13(10)16/h1-2,4,7-8,13,16H,3,5-6H2,(H,14,15)-810+10
    키: UADPGHINQMWEAG-CSKARUKUBJ
  • c1cc2c(c1)CC/C(=C\C(=O)O)/C2O
특성.
C13H14O3
몰 질량 218.248
달리 명시되지 않은 한 표준 상태(25°C[77°F], 100kPa)의 재료에 대한 데이터가 제공됩니다.

NCS-382는 GHB [1][2]수용체에 대한 중간 선택성 길항제이다.동물에 대한 GHB의 영향을 차단하고 항진정 및 항경련 [3][4][5]효과가 있습니다.인간의 GHB 과다 복용 및 유전대사 장애인 숙신산세미알데히드탈수소효소결핍증(SSADHD)에 대한 치료제로 제안되었지만 임상용으로 [6]개발된 적은 없다.

레퍼런스

  1. ^ Castelli MP, Pibiri F, Carboni G, Piras AP (2004). "A review of pharmacology of NCS-382, a putative antagonist of gamma-hydroxybutyric acid (GHB) receptor". CNS Drug Reviews. 10 (3): 243–260. doi:10.1111/j.1527-3458.2004.tb00025.x. PMC 6741708. 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 (1): 374–385. Bibcode:2008NYASA1139..374T. doi:10.1196/annals.1432.048. PMID 18991884.
  3. ^ Maitre M, Hechler V, Vayer P, Gobaille S, Cash CD, Schmitt M, Bourguignon JJ (Nov 1990). "A specific gamma-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties". Journal of Pharmacology and Experimental Therapeutics. 255 (2): 657–63. PMID 2173754.
  4. ^ Schmidt C, Gobaille S, Hechler V, Schmitt M, Bourguignon JJ, Maitre M (Oct 1991). "Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist". European Journal of Pharmacology. 203 (3): 393–7. doi:10.1016/0014-2999(91)90896-X. PMID 1773824.
  5. ^ Colombo G, Agabio R, Bourguignon J, Fadda F, Lobina C, Maitre M, Reali R, Schmitt M, Gessa GL (Sep 1995). "Blockade of the discriminative stimulus effects of gamma-hydroxybutyric acid (GHB) by the GHB receptor antagonist NCS-382". Physiology & Behavior. 58 (3): 587–590. doi:10.1016/0031-9384(95)00086-X. PMID 8587968.
  6. ^ Gupta M, Greven R, Jansen EE, Jakobs C, Hogema BM, Froestl W, Snead OC, Bartels H, Grompe M, Gibson KM (Jul 2002). "Therapeutic intervention in mice deficient for succinate semialdehyde dehydrogenase (gamma-hydroxybutyric aciduria)". Journal of Pharmacology and Experimental Therapeutics. 302 (1): 180–187. doi:10.1124/jpet.302.1.180. PMID 12065715.