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A-α-CAO对小鼠(icv)具有弱而短暂的镇痛作用并能拮抗吗啡(Mor)镇痛效应3—4d。未见A-α-CAO有成瘾倾向。小鼠输精管(MVD)试验表明A-α-CAO为阿片受点部分激剂,Ke为9×10~(-9)mol/L。保温时间较长或剂量较大,其拮抗效应经多次冲洗仍然存在,激剂作用亦不能被纳洛酮(N_x)翻转。A-α-CAO对豚鼠回肠纵肌(GPI)呈完全激剂效应,IC_(50)为5.7×10~(-10)mol/L,冲洗不能除去此种作用,但可被N_x翻转。在大鼠输精管(RVD)和兔输精管(RbVD)上A-α-CAO呈抗剂效应,pA_2值分别为7.5和7.6,作用也不易被冲洗除去。A-α-CAO可抑制~3H-依托啡(~3H-Etor)与小鼠脑勻浆P_2制备的特异给合,IC_(50)为3.2×10~(-9)mol/L,冲洗6次后A-α-CAO对~3H-Etor高亲合力结合的抑制仍达96％。
A-α-CAO has a weak and transient analgesic effect on mice (icv) and antagonizes morphine (Mor) analgesic effect 3-4d. No A-α-CAO is found to be addictive. Mouse vas deferens (MVD) test showed that A-α-CAO is a partial ophthalmic agonist, Ke is 9 × 10 -9 mol / L. Insulation time longer or larger dose, the antagonistic effect after multiple flushing still exist, the agonist can not be reversed by naloxone (N_x). A-α-CAO showed a complete agonist effect on guinea pig ileum longitudinal muscle (GPI) with an IC50 of 5.7 × 10 -10 mol / L. Flushing could not remove this effect but was reversed by N_x. A-α-CAO showed an anti-agent effect on rat vas deferens (RVD) and rabbit vas deferens (RbVD), with pA_2 values of 7.5 and 7.6, respectively. A-α-CAO inhibited the specific administration of ~ 3H-Etor and mouse brain homogenate P_2 with IC50 of 3.2 × 10 -9 mol / L, Secondary A-α-CAO inhibition of ~ 3H-Etor high affinity binding still reached 96%.