베다클리딘

Vedaclidine
베다클리딘
Vedaclidine.svg
Vedaclidine 3D.png
임상 데이터
기타 이름(S)-3-[4-(부틸티오)-1, 2, 5-티아디아졸-3-일]퀴뉴클리딘
ATC 코드
  • 없음.
식별자
  • (3S)-3-[4-(부틸술파닐)-1, 2, 5-티아디아졸-3-일]퀴니딘
CAS 번호
PubChem CID
켐스파이더
유니
첸블
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C13H21N3S2
몰 질량283.45 g/g−1/g
3D 모델(JSmol)
  • CCCSC1=NSN=C1[C@@H]2CN3CC2CC3
  • InChI=1S/C13H21N3S2/c1-2-3-8-17-13-12(14-18-15-13)11-9-16-6-4-10(11)5-7-16/h10-11H, 2-9H2, 1H3/1/s
  • 키: WZPXVUFFDJHGI-LLVKDONJSA-N

베다클리딘([1]: 180 Vedaclidine, 코드네임 LY-297,802, NNC 11-1053)은 무스카린성 아세틸콜린 수용체에서 혼합작용제-항작용제로 작용하는 실험용 진통제이며, M, M43,[2][3] M5 서브타입에서는2 강력하고1 선택적인 작용제이지만, M, M 서브타입에서는 길항제이다.구강 활성으로 모르핀의 3배 이상의 효능을 가지며, 침과 떨림과 같은 부작용은 효과적인 진통제 [4][5][6]복용량의 몇 배에서만 발생한다.인체 실험은 의존성이나 [7]남용의 발생 가능성을 거의 보여주지 않았으며, 신경성 통증과 암 통증 [8]완화에 가능한 임상적 응용에 대한 연구는 계속되고 있다.

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레퍼런스

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 38" (PDF). World Health Organization. 1997. Retrieved 18 November 2016.
  2. ^ Shannon HE, Womer DE, Bymaster FP, Calligaro DO, DeLapp NC, Mitch CH, et al. (1997). "In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist". Life Sciences. 60 (13–14): 969–76. doi:10.1016/s0024-3205(97)00036-2. PMID 9121363.
  3. ^ Womer DE, Shannon HE (September 2000). "Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice". Neuropharmacology. 39 (12): 2499–504. doi:10.1016/S0028-3908(00)00068-X. PMID 10974334. S2CID 31065787.
  4. ^ Swedberg MD, Sheardown MJ, Sauerberg P, Olesen PH, Suzdak PD, Hansen KT, et al. (May 1997). "Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic". The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 876–83. PMID 9152397.
  5. ^ Shannon HE, Sheardown MJ, Bymaster FP, Calligaro DO, Delapp NW, Gidda J, et al. (May 1997). "Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053): a novel analgesic with mixed muscarinic receptor agonist and antagonist activity". The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 884–94. PMID 9152398.
  6. ^ Shannon HE, Jones CK, Li DL, Peters SC, Simmons RM, Iyengar S (September 2001). "Antihyperalgesic effects of the muscarinic receptor ligand vedaclidine in models involving central sensitization in rats". Pain. 93 (3): 221–7. doi:10.1016/S0304-3959(01)00319-0. PMID 11514081. S2CID 10256837.
  7. ^ Petry NM, Bickel WK, Huddleston J, Tzanis E, Badger GJ (April 1998). "A comparison of subjective, psychomotor and physiological effects of a novel muscarinic analgesic, LY297802 tartrate, and oral morphine in occasional drug users". Drug and Alcohol Dependence. 50 (2): 129–36. doi:10.1016/S0376-8716(98)00026-X. PMID 9649964.
  8. ^ Tata AM (June 2008). "Muscarinic acetylcholine receptors: new potential therapeutic targets in antinociception and in cancer therapy". Recent Patents on CNS Drug Discovery. 3 (2): 94–103. doi:10.2174/157488908784534621. PMID 18537768.