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羟甲芬太尼(F 7302,N-[1-(β-羟基-β-苯乙基)-3-甲基-4-哌啶基]-N-丙酰苯胺)是一个合成的强效镇痛剂,小鼠上的镇痛强度为吗啡的 6300倍.Na~+(100 mM)和 GTP(50 μM)可以减少羟甲芬太尼抑制~3H-naloxone特异性结合的强度,指出这个化合物呈现阿片激动剂性质.~3H-羟甲芬太尼与小鼠脑匀浆P_2部分阿片受体的结合具有饱和性、专一性和可逆性,Scatchard分析指出两个不同的结合点(K_(D1)=0.32nM,K_(D2)=3.91nM).各种阿片类药物可以较强地抑制~3H-羟甲芬太尼的特异性结合,而非阿片类药物不能抑制这种结合.比较吗啡、DSTLE和羟甲芬太尼抑制~3H-di-hydromorphine(μ)和’~3H-[D-Ala~2,D-Leu~5]enkephalin(δ)结合到小鼠脑突触浆膜阿片受体上的强度,结果表明,吗啡、DSTLE和羟甲芬太尼抑制~3H-dihydromorphine(μ)结合的强度分别为抑制~3H-[D-Ala~2,D-Leu~5]-enkephalin(δ)结合强度的79,0.11和81.5倍,从而提示羟甲芬太尼是一个强的μ激动剂。
Hydroxymetazidine (F 7302, N- [1- (β-hydroxy-β-phenylethyl) -3-methyl-4-piperidinyl] propionanilide) is a potent and potent Analgesic, the analgesic strength in mice is 6300 times that of morphine.Na ~ + (100 mM) and GTP (50 μM) can reduce the intensity of oxymetazidine inhibition of ~ 3H-naloxone-specific binding, pointing out that this The compounds showed opiate agonist properties. ~ 3H-Hydroxymefentanil was partially saturated, specific, and reversible in binding to some P opioid receptors in brain homogenates of mice. Scatchard analysis showed that two different binding sites (K_ (D1) = 0.32 nM, K D2 = 3.91 nM) .A variety of opioids can strongly inhibit the specific binding of 3H-hydroxymethafentanil, while non-opioids can not inhibit this binding. Compared with morphine, DSTLE and oxymetazidine inhibited the binding of ~ 3H-di-hydromorphine (μ) and ~ 3H- [D-Ala ~ 2, D-Leu ~ 5] enkephalin (δ) The results showed that the inhibitory effect of morphine, DSTLE and oxymetazidine on the inhibition of 3H-dihydromorphine (μ) binding was ~ 3H- [D-Ala ~ 2, D-Leu ~ 5] -enkephalin (δ) binding strengths of 79,0.11 and 81.5 times, suggesting that oxymetapane is a strong μ agonist.