Vedaclidine

Vedaclidine
Systematic (IUPAC) name
	(3-(3-1-butylthio)-1,2,5-thiadiazol-4-yl)-1-azabicyclo-2.2.2-octane
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	141575-52-2
ATC code	None
PubChem	CID 60868
ChemSpider	54852
UNII	98IW5HAV1N
Chemical data
Formula	C13H21N3S2
Mol. mass	283.455 g/mol
SMILES	eMolecules & PubChem

Vedaclidine (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.^[1]^[2] It is orally active and an effective analgesic over 3x the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose.^[3]^[4]^[5] Human trials showed little potential for development of dependence or abuse,^[6] and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.^[7]

[edit] See also

[edit] References

^ 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. In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist. Life Sciences. 1997;60(13-14):969-76. 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, Mitch CH, Calligaro DO, Delapp NW, Shannon HE. Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic. Journal Pharmacology and Experimental Therapeutics. 1997 May;281(2):876-83. PMID 9152397
^ 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. 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. 1997 May;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.

[0] 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. In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist. Life Sciences. 1997;60(13-14):969-76. PMID 9121363

[1] 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.

[2] Swedberg MD, Sheardown MJ, Sauerberg P, Olesen PH, Suzdak PD, Hansen KT, Bymaster FP, Ward JS, Mitch CH, Calligaro DO, Delapp NW, Shannon HE. Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic. Journal Pharmacology and Experimental Therapeutics. 1997 May;281(2):876-83. PMID 9152397

[3] 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. 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. 1997 May;281(2):884-94. PMID 9152398

[4] 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.

[5] 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.

[6] 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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Mar	APR	May
	01
2011	2012	2013

Vedaclidine

[edit] See also

[edit] References

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