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, H. E.; Womer, D. E.; Bymaster, F. P.; Calligaro, D. O.; Delapp, N. C.; Mitch, C. H.; Ward, J. S.; Whitesitt, C. A.; Swedberg, M. D.; Sheardown, M. J.; Fink-Jensen, A.; Olesen, P. H.; Rimvall, K.; Sauerberg, P. (1997). „In vivo pharmacology of butylthio2.2.2 (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist”. Life Sciences. 60 (13–14): 969—976. PMID 9121363. doi:10.1016/s0024-3205(97)00036-2. }-
^ Womer DE, Shannon HE (2000). „Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists in mice”. 39 (12): 2499—504. PMID 10974334. doi:10.1016/S0028-3908(00)00068-X.
^ Swedberg, M. D.; Sheardown, M. J.; Sauerberg, P.; Olesen, P. H.; Suzdak, P. D.; Hansen, K. T.; Bymaster, F. P.; Ward, J. S.; Mitch, C. H.; Calligaro, D. O.; Delapp, N. W.; Shannon, H. E. (1997). „Butylthio2.2.2 (NNC 11-1053/LY297802): An orally active muscarinic agonist analgesic”. The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 876—883. PMID 9152397. doi:10.1016/S0022-3565(24)36644-3. }-
^ Shannon, H. E.; Sheardown, M. J.; Bymaster, F. P.; Calligaro, D. O.; Delapp, N. W.; Gidda, J.; Mitch, C. H.; Sawyer, B. D.; Stengel, P. W.; Ward, J. S.; Wong, D. T.; Olesen, P. H.; Suzdak, P. D.; Sauerberg, P.; Swedberg, M. D. (1997). „Pharmacology of butylthio2.2.2 (LY297802/NNC11-1053): A novel analgesic with mixed muscarinic receptor agonist and antagonist activity”. The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 884—894. PMID 9152398. doi:10.1016/S0022-3565(24)36645-5. }-
^ 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”. 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”. 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”. 3 (2): 94—103. PMID 18537768. doi:10.2174/157488908784534621.

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[1] Shannon, H. E.; Womer, D. E.; Bymaster, F. P.; Calligaro, D. O.; Delapp, N. C.; Mitch, C. H.; Ward, J. S.; Whitesitt, C. A.; Swedberg, M. D.; Sheardown, M. J.; Fink-Jensen, A.; Olesen, P. H.; Rimvall, K.; Sauerberg, P. (1997). „In vivo pharmacology of butylthio2.2.2 (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist”. Life Sciences. 60 (13–14): 969—976. PMID 9121363. doi:10.1016/s0024-3205(97)00036-2. }-

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

[3] Swedberg, M. D.; Sheardown, M. J.; Sauerberg, P.; Olesen, P. H.; Suzdak, P. D.; Hansen, K. T.; Bymaster, F. P.; Ward, J. S.; Mitch, C. H.; Calligaro, D. O.; Delapp, N. W.; Shannon, H. E. (1997). „Butylthio2.2.2 (NNC 11-1053/LY297802): An orally active muscarinic agonist analgesic”. The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 876—883. PMID 9152397. doi:10.1016/S0022-3565(24)36644-3. }-

[4] Shannon, H. E.; Sheardown, M. J.; Bymaster, F. P.; Calligaro, D. O.; Delapp, N. W.; Gidda, J.; Mitch, C. H.; Sawyer, B. D.; Stengel, P. W.; Ward, J. S.; Wong, D. T.; Olesen, P. H.; Suzdak, P. D.; Sauerberg, P.; Swedberg, M. D. (1997). „Pharmacology of butylthio2.2.2 (LY297802/NNC11-1053): A novel analgesic with mixed muscarinic receptor agonist and antagonist activity”. The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 884—894. PMID 9152398. doi:10.1016/S0022-3565(24)36645-5. }-

[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”. 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”. 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”. 3 (2): 94—103. PMID 18537768. doi:10.2174/157488908784534621.

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