Vedaclidine

Vedaclidine (INN,[1]:180 codenamed LY-297,802, NNC 11-1053) is a novel analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes.[2][3] It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose.[4][5][6] Human trials showed little potential for development of dependence or abuse,[7] and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.[8]

Vedaclidine
Clinical data
Other names(S)-3-[4-(butylthio)-1,2,5-thiadiazol-3-yl]quinuclidine
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC13H21N3S2
Molar mass283.45 g·mol−1
3D model (JSmol)

See also

References
  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.
  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.
  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.
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