GS-39783

GS-39783
GS-39783
GS-39783 structure.png
식별자
  • N, N-디시클로펜틸파닐-5-니트로피리미딘-4,6-다이아민
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
CompTox 대시보드 (EPA)
ECHA InfoCard100.164.558 Edit this at Wikidata
화학 및 물리적 데이터
공식C15H23N5O2S
어금질량337.44 g·190−1
3D 모델(JSmol)
  • C3CCC3Nc1nc(SC)nc(=O)=O)NC2CCC2
  • InChI=1S/C15H23N5O2S/c1-23-15-18-13(16-10-6-2-3-7-10)12(20(21)22)14(19-15)17-11-8-4-5-9-11/h10-11H,2-9H2,1H3,(H2,16,17,18,19) ☒N
  • 키:GSGVDKOCBKBMG-UHFFFAOYSA-N ☒N
☒NcheckY (이게 뭐야?) (iii)

GS-39783은 GABAB 수용체에서 양성 알로스테릭 모듈레이터 역할을 하는 과학 연구에 사용되는 화합물이다.[1][2]동물 연구에서 항불안제 효과를 발생시키고,[3][4][5] 알코올,[6][7] 코카인[8][9][10], 니코틴의 자가 투여를 감소시키는 것으로 나타났다.[11]null

참조

  1. ^ Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, et al. (October 2003). "N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function". The Journal of Pharmacology and Experimental Therapeutics. 307 (1): 322–30. doi:10.1124/jpet.103.053074. PMID 12954816.
  2. ^ Guery S, Floersheim P, Kaupmann K, Froestl W (November 2007). "Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors". Bioorganic & Medicinal Chemistry Letters. 17 (22): 6206–11. doi:10.1016/j.bmcl.2007.09.023. PMC 2278029. PMID 17884493.
  3. ^ Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF (June 2004). "Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior". Neuropsychopharmacology. 29 (6): 1050–62. doi:10.1038/sj.npp.1300413. PMID 15039762.
  4. ^ Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, et al. (September 2004). "Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines". The Journal of Pharmacology and Experimental Therapeutics. 310 (3): 952–63. doi:10.1124/jpet.104.066753. PMID 15113848.
  5. ^ Jacobson LH, Cryan JF (April 2008). "Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents". Neuropharmacology. 54 (5): 854–62. doi:10.1016/j.neuropharm.2008.01.004. PMID 18328507.
  6. ^ Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, et al. (November 2005). "Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats". European Journal of Pharmacology. 525 (1–3): 105–11. doi:10.1016/j.ejphar.2005.10.005. PMID 16289452.
  7. ^ Maccioni P, Pes D, Orrù A, Froestl W, Gessa GL, Carai MA, Colombo G (August 2007). "Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats". Psychopharmacology. 193 (2): 171–8. doi:10.1007/s00213-007-0776-1. PMID 17393141.
  8. ^ Smith MA, Yancey DL, Morgan D, Liu Y, Froestl W, Roberts DC (April 2004). "Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats". Psychopharmacology. 173 (1–2): 105–11. doi:10.1007/s00213-003-1706-5. PMID 14712341.
  9. ^ Slattery DA, Markou A, Froestl W, Cryan JF (November 2005). "The GABAB receptor-positive modulator GS39783 and the GABAB receptor agonist baclofen attenuate the reward-facilitating effects of cocaine: intracranial self-stimulation studies in the rat". Neuropsychopharmacology. 30 (11): 2065–72. doi:10.1038/sj.npp.1300734. PMID 15841108.
  10. ^ Lhuillier L, Mombereau C, Cryan JF, Kaupmann K (February 2007). "GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine". Neuropsychopharmacology. 32 (2): 388–98. doi:10.1038/sj.npp.1301102. PMC 1774586. PMID 16710312.
  11. ^ Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A (July 2008). "Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats". The Journal of Pharmacology and Experimental Therapeutics. 326 (1): 306–14. doi:10.1124/jpet.108.139204. PMC 2574924. PMID 18445779.