ベダクリジン

ベダクリジン
IUPAC命名法による物質名
	IUPAC名 (3-(3-1-Butylthio)-1,2,5-thiadiazol-4-yl)-1-azabicyclo[2.2.2]octane;
識別
CAS番号;	141575-52-2
ATCコード	None
PubChem	CID: 60868
ChemSpider	54852
UNII	98IW5HAV1N
化学的データ
化学式	C13H21N3S2
分子量	283.455 g/mol
	SMILES C3CC1CCN3CC1c2nsnc2SCCCC;
	テンプレートを表示

ベダクリジン(Vedaclidine)は、ムスカリン性アセチルコリン受容体のアゴニスト及びアンタゴニストとして作用する鎮痛剤である。M₁型及びM₄型の強力な選択的アゴニスト、M₂型、M₃型、M₅型のアンタゴニストとなる^[1]^[2]。モルヒネの3倍以上強力な経口鎮痛剤であり、流涎や震え等の副作用は、有効量の何倍も服用した時にしか生じない^[3]^[4]^[5]。ヒトの臨床試験では、依存性はほとんど見られず^[6]、神経因性疼痛や癌性疼痛の緩和のための医療現場での利用に向けた研究が続いている^[7]。

出典

^ 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.

[1] 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.

[2] 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.

[3] 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.

[4] 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.

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

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

[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. doi:10.2174/157488908784534621. PMID 18537768.

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関連項目

出典