Vedaclidine
 | |
| Clinical data | |
|---|---|
| ATC code | None |
| Identifiers | |
| |
| Synonyms | (S)-3-[4-(butylthio)-1,2,5-thiadiazol-3-yl]quinuclidine |
| CAS Number | 141575-52-2 |
| PubChem (CID) | 9889093 |
| ChemSpider | 8064764 |
| UNII |
98IW5HAV1N  |
| ChEMBL | CHEMBL136807 |
| Chemical and physical data | |
| Formula | C13H21N3S2 |
| Molar mass | 283.455 g/mol |
| 3D model (Jmol) | Interactive image |
| |
| |
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]
See also
References
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 38" (PDF). World Health Organization. 1997. Retrieved 18 November 2016.
- ↑ Shannon, HE; Womer, DE; Bymaster, FP; Calligaro, DO; DeLapp, NC; Mitch, CH; Ward, JS; Whitesitt, CA; 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.
- ↑ Womer, DE; Shannon, HE (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.
- ↑ Swedberg, MD; Sheardown, MJ; Sauerberg, P; Olesen, PH; Suzdak, PD; Hansen, KT; Bymaster, FP; Ward, JS; et al. (May 1997). "Butylthio[2.2.2] (NNC 11-1053/LY297802) an orally active muscarinic agonist analgesic". Journal Pharmacology and Experimental Therapeutics. 281 (2): 876–83. PMID 9152397.
- ↑ Shannon, HE; Sheardown, MJ; Bymaster, FP; Calligaro, DO; Delapp, NW; Gidda, J; Mitch, CH; Sawyer, BD; et al. (May 1997). "Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053) a novel analgesic with mixed muscarinic receptor agonist and antagonist activity". Journal of Pharmacology and Experimental Therapeutics. 281 (2): 884–94. PMID 9152398.
- ↑ Shannon, HE; Jones, CK; Li, DL; Peters, SC; Simmons, RM; Iyengar, S (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.
- ↑ Petry, NM; Bickel, WK; Huddleston, J; Tzanis, E; Badger, GJ (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.
- ↑ Tata, AM (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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