Chemistry:Vedaclidine
From HandWiki
Short description: Chemical compound
 | |
 | |
| Clinical data | |
|---|---|
| Other names | (S)-3-[4-(butylthio)-1,2,5-thiadiazol-3-yl]quinuclidine |
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C13H21N3S2 |
| Molar mass | 283.45 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Vedaclidine (INN,[1]:180 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
References
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 38". World Health Organization. 1997. https://www.who.int/medicines/publications/druginformation/innlists/RL38.pdf.
- ↑ "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. doi:10.1016/s0024-3205(97)00036-2. PMID 9121363.
- ↑ "Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice". Neuropharmacology 39 (12): 2499–504. September 2000. doi:10.1016/S0028-3908(00)00068-X. PMID 10974334.
- ↑ "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. PMID 9152397.
- ↑ "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. PMID 9152398.
- ↑ "Antihyperalgesic effects of the muscarinic receptor ligand vedaclidine in models involving central sensitization in rats". Pain 93 (3): 221–7. September 2001. doi:10.1016/S0304-3959(01)00319-0. PMID 11514081.
- ↑ "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. doi:10.1016/S0376-8716(98)00026-X. PMID 9649964.
- ↑ "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. doi:10.2174/157488908784534621. PMID 18537768.
 |  |
