产品
编 号：F618147
分子式：C20H26N2O9
分子量：438.43
分子式：C20H26N2O9
分子量：438.43
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CAS No: 2454492-41-0
产品详情
生物活性：
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 μM. Antinociceptive effect.
体内研究：
TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice.TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats.Animal Model:Adult male mice (body weight 15-30 g) (formalin test)
Dosage:1, 3, 10 mg/kg
Administration:I.p.
Result:Dose dependently reduced both early and late phases of formalin induced nociceptive behavioral responses.
Animal Model:Adult male SD rats (body weight 200-220 g) (chronic constriction injury (CCI))
Dosage:0.3, 1, 3 mg/kg
Administration:I.p.
Result:Significantly reversed CCI induced the paw withdrawal threshold decreases.
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 μM. Antinociceptive effect.
体内研究：
TC-2559 difumarate (1-10 mg/kg; i.p.) dose dependently reduces acute formalin-induced biphasic nociceptive responses in mice.TC-2559 difumarate (0.3-3 mg/kg; i.p.) dose dependently inhibits CCI-induced neuropathic pain in rats.Animal Model:Adult male mice (body weight 15-30 g) (formalin test)
Dosage:1, 3, 10 mg/kg
Administration:I.p.
Result:Dose dependently reduced both early and late phases of formalin induced nociceptive behavioral responses.
Animal Model:Adult male SD rats (body weight 200-220 g) (chronic constriction injury (CCI))
Dosage:0.3, 1, 3 mg/kg
Administration:I.p.
Result:Significantly reversed CCI induced the paw withdrawal threshold decreases.
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