Vedaclidine Explained

Vedaclidine (INN,[1] codenamed LY-297,802, NNC 11-1053) is an experimental 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]

See also

Notes and References

  1. Web site: International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 38 . World Health Organization . 18 November 2016 . 1997.
  2. Shannon HE, Womer DE, Bymaster FP, Calligaro DO, DeLapp NC, Mitch CH, Ward JS, Whitesitt CA, Swedberg MD, Sheardown MJ, Fink-Jensen A, Olesen PH, Rimvall K, Sauerberg P . 6 . In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist . Life Sciences . 60 . 13–14 . 969–76 . 1997 . 9121363 . 10.1016/s0024-3205(97)00036-2 .
  3. Womer DE, Shannon HE . Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice . Neuropharmacology . 39 . 12 . 2499–504 . September 2000 . 10974334 . 10.1016/S0028-3908(00)00068-X . 31065787 .
  4. Swedberg MD, Sheardown MJ, Sauerberg P, Olesen PH, Suzdak PD, Hansen KT, Bymaster FP, Ward JS, Mitch CH, Calligaro DO, Delapp NW, Shannon HE . 6 . 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 . May 1997 . 9152397 .
  5. Shannon HE, Sheardown MJ, Bymaster FP, Calligaro DO, Delapp NW, Gidda J, Mitch CH, Sawyer BD, Stengel PW, Ward JS, Wong DT, Olesen PH, Suzdak PD, Sauerberg P, Swedberg MD . 6 . 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 . May 1997 . 9152398 .
  6. Shannon HE, Jones CK, Li DL, Peters SC, Simmons RM, Iyengar S . Antihyperalgesic effects of the muscarinic receptor ligand vedaclidine in models involving central sensitization in rats . Pain . 93 . 3 . 221–7 . September 2001 . 11514081 . 10.1016/S0304-3959(01)00319-0 . 10256837 .
  7. Petry NM, Bickel WK, Huddleston J, Tzanis E, Badger GJ . 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 . April 1998 . 9649964 . 10.1016/S0376-8716(98)00026-X .
  8. Tata AM . Muscarinic acetylcholine receptors: new potential therapeutic targets in antinociception and in cancer therapy . Recent Patents on CNS Drug Discovery . 3 . 2 . 94–103 . June 2008 . 18537768 . 10.2174/157488908784534621 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Vedaclidine".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.