Vedaklidin

Vedaklidin
IUPAC ime
	(3-(3-1-butiltio)-1,2,5-tiadiazol-4-il)-1-azabiciklo-2.2.2-oktan
Identifikatori
CAS broj	141575-52-2
ATC kod	None
PubChem	CID 60868
ChemSpider	54852
UNII	98IW5HAV1N
Hemijski podaci
Formula	C13H21N3S2
Molarna masa	283,455 g/mol
	SMILES C3CC1CCN3CC1c2nsnc2SCCCC; ;

Vedaklidin (LY-297,802, NNC 11-1053) je analgetski lek koji deluje kao mešoviti agonist-antagonist na muscarinskim acetilholinskim receptorima. On je potentan i selektivan agonist na M₁ i M₄ podtipovima, a antagonist na M₂, M₃ i M₅ podtipovima.^[1]^[2] Vedaklidin je oralno aktivan i efektivan analgetik, koji je više od tri puta potentniji od morfina. Njegove nuspojave su salivacija i tremor, koje se javljaju pri dozama koje su nekoliko puta veće od efektivne.^[3]^[4]^[5] Klinička ispitivanja su pokazala da on ima neznatan potencijal za razvoj zavisnosti ili zloupotrebu.^[6] Dalja ispitivanja s ciljem utvđivanja moguće kliničke primene u tretiranju neuropatičkog bola i olakšavanja bola uzrokovanog kancerom su u toku.^[7]

Reference

^ 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. PMID 10974334. doi:10.1016/S0028-3908(00)00068-X.
^ 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. PMID 11514081. doi:10.1016/S0304-3959(01)00319-0.
^ 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. PMID 9649964. doi:10.1016/S0376-8716(98)00026-X.
^ 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. PMID 18537768. doi:10.2174/157488908784534621.

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[1] 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

[2] Womer DE, Shannon HE (2000). „Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice”. Neuropharmacology. 39 (12): 2499—504. PMID 10974334. doi:10.1016/S0028-3908(00)00068-X.

[3] 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

[4] 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

[5] 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. PMID 11514081. doi:10.1016/S0304-3959(01)00319-0.

[6] 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. PMID 9649964. doi:10.1016/S0376-8716(98)00026-X.

[7] 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. PMID 18537768. doi:10.2174/157488908784534621.

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