RS-10221

RS-102221
RS-10221
RS-102,221 structure.png
임상자료
기타 이름RS-102,221; 8-[2,4-디메톡시-5- (4-트리플루오르메틸펜실술포나미도)페닐 -5-옥소펜틸]-1,3,8-트리아자스피로[4.5]데케인-2,4-디오네
식별자
  • N-{{{5-[2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl] -2,4-dimethoxoxyphenyl}-4-(트리플루오로메틸)벤젠설폰아미드
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
켐벨
화학 및 물리적 데이터
공식C27H33F3N4O7S
어금질량614.64 g·migration−1
3D 모델(JSmol)
  • c4cc(C(F)F)cc4S(=O)Nc(C(OC)cc2OC)CC2C(=O)CCCN(CC3)CC13NC(=O)NC1=O
  • InChI=1S/C27H31F3N4O7S/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37)
  • 키:HZZZODVDSHQRG-UHFFFAOYSA-N
☒NcheckY (이게 뭐야?) (iii)

RS-10221은 호프만-라 로슈가 개발한 약물로, 세로토닌 5-HT2C 수용체에서 강력한 선택적 길항제 역할을 하는 화합물 중 하나로 밀접하게 연관된 5-HT2A 수용체 및 5-HT2B 수용체보다 약 100배 선택성이 있다.[1] 동물 연구에서 항불안제 효과가 [2]있고 SSRI 항우울제의 효능이 [3]증가하며 코카인과의 복잡한 상호작용을 보여 일부 효과는 증가하나 다른 것은 감소시켜 뇌의 도파민 신호전달계통 조절에 있어 5-HT2C 수용체에 대한 역할을 반영한다.[4][5][6][7]

참고 항목

참조

  1. ^ Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, et al. (1997). "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology. 36 (4–5): 621–9. doi:10.1016/s0028-3908(97)00049-x. PMID 9225287. S2CID 24930608.
  2. ^ Kuznetsova EG, Amstislavskaya TG, Shefer EA, Popova NK (July 2006). "Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior". Bulletin of Experimental Biology and Medicine. 142 (1): 76–9. doi:10.1007/s10517-006-0296-8. PMID 17369908. S2CID 36424571.
  3. ^ Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, et al. (October 2004). "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology. 29 (10): 1782–9. doi:10.1038/sj.npp.1300474. PMID 15138437.
  4. ^ Filip M, Cunningham KA (April 2002). "Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus effects of cocaine". Pharmacology, Biochemistry, and Behavior. 71 (4): 745–56. doi:10.1016/s0091-3057(01)00741-9. PMID 11888566. S2CID 292398.
  5. ^ Filip M, Cunningham KA (August 2003). "Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex". The Journal of Pharmacology and Experimental Therapeutics. 306 (2): 734–43. doi:10.1124/jpet.102.045716. PMID 12721337. S2CID 8338748.
  6. ^ Morita K, Hamamoto M, Arai S, Kitayama S, Irifune M, Kawahara M, et al. (September 2005). "Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities" (PDF). Brain Research. 1057 (1–2): 153–60. doi:10.1016/j.brainres.2005.07.049. PMID 16125150. S2CID 30437231.
  7. ^ Dremencov E, Weizmann Y, Kinor N, Gispan-Herman I, Yadid G (February 2006). "Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response". Current Drug Targets. 7 (2): 165–75. doi:10.2174/138945006775515491. PMID 16475958.