Colombo G, Agabio R, Lobina C, Reali R, Gessa G L
C.N.R. Center for Neuropharmacology, Cagliari, Italy.
Eur J Pharmacol. 1998 Feb 26;344(1):67-9. doi: 10.1016/s0014-2999(97)01555-0.
The effect of cannabinoid receptor activation and blockade on the propulsive activity in the mouse small intestine was assessed in the present study by measuring the transit of an orally administered, non-absorbable marker. The cannabinoid receptor agonist WIN 55,212-2 (R(+)-[2,3-dihydro-5-methyl-3[(morpholinyl)methyl]pyrrolo[1,2,3-de-1, 4benzoxazin-yl]-(1-naphthalenyl)methanone mesylate) inhibited, while the selective cannabinoid CB1 receptor antagonist SR 141716A (N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyraz ole-carboxamide) stimulated the marker transit. Furthermore, a per se non-effective dose of SR 141716A reversed WIN 55,212-2-induced reduction of the transit. The results of the present study suggest a role for cannabinoid CB1 receptors in the control of propulsive activity in the mouse small intestine.
在本研究中,通过测量口服非吸收性标记物的转运情况,评估了大麻素受体激活和阻断对小鼠小肠推进活动的影响。大麻素受体激动剂WIN 55,212-2(R(+)-[2,3-二氢-5-甲基-3-[(吗啉基)甲基]吡咯并[1,2,3-de-1,4]苯并恶嗪基]-(1-萘基)甲酮甲磺酸盐)具有抑制作用,而选择性大麻素CB1受体拮抗剂SR 141716A(N-哌啶基-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-3-吡唑甲酰胺)则刺激标记物转运。此外,本身无效应剂量的SR 141716A可逆转WIN 55,212-2引起的转运减少。本研究结果表明,大麻素CB1受体在小鼠小肠推进活动的控制中发挥作用。