212332-35-9
中文名稱(chēng)
4-(5-ETHOXY-3-PYRIDINYL)-N-METHYL-(3E)-3-BUTEN-1-AMINE DIFUMARATE
CAS
212332-35-9
分子式
C20H26N2O9
MOL 文件
212332-35-9.mol
212332-35-9 結(jié)構(gòu)式
基本信息
英文別名
TC 2559 (fumarate)TC 2559 DIFUMARATE
4-(5-ETHOXY-3-PYRIDINYL)-N-METHYL-(3E)-3-BUTEN-1-AMINE DIFUMARATE
常見(jiàn)問(wèn)題列表
生物活性
TC-2559 difumarate 是 CNS 選擇性，具有口服活性的煙堿乙酰膽堿受體 (nAChR) α4β2 亞型的部分激動(dòng)劑。TC-2559 difumarate 對(duì) α2β4、α4β4 和 α3β4 受體表現(xiàn)出選擇性，EC50在 10-30 μM 范圍內(nèi)。體內(nèi)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. |