首页> 外文期刊>European Journal of Pharmacology: An International Journal >Benzophenanthridine alkaloid, piperonyl butoxide and (S)-methoprene action at the cannabinoid-1 receptor (CB_1-receptor) pathway of mouse brain: Interference with [~3H]CP55940 and [~3H]SR141716A binding and modification of WIN55212-2-dependent inhibition of synaptosomal L-glutamate release
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Benzophenanthridine alkaloid, piperonyl butoxide and (S)-methoprene action at the cannabinoid-1 receptor (CB_1-receptor) pathway of mouse brain: Interference with [~3H]CP55940 and [~3H]SR141716A binding and modification of WIN55212-2-dependent inhibition of synaptosomal L-glutamate release

机译:苯并菲啶生物碱,胡椒基丁醚和(S)-甲蝶呤对小鼠大脑大麻素1受体(CB_1-受体)途径的作用:干扰[〜3H] CP55940和[〜3H] SR141716A结合和修饰WIN55212-2依赖性抑制突触体谷氨酸释放

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摘要

Benzophenanthridine alkaloids (chelerythrine and sanguinarine) inhibited binding of [~3H]SR141716A to mouse brain membranes (IC_50s: < 1 uM). Piperonyl butoxide and (S)-methoprene were less potent (IC_50s: 21 and 63 uM respectively). Benzophenanthridines and piperonyl butoxide were more selective towards brain CB_1 receptors versus spleen CB_2 receptors. All compounds reduced B_(max) of [~3H]SR141716A binding to CB_1 receptors, but only methoprene and piperonyl butoxide increased K_d (3-5-fold). Benzophenanthridines increased the K_d of [~3H]CP55940 binding (6-fold), but did not alter B_(max). (S)-methoprene increased the K_d of [~3H]CP55940 binding (by almost 4-fold) and reduced B_(max) by 60%.
机译:苯并菲啶生物碱(白屈菜红碱和血红碱碱)抑制[〜3H] SR141716A与小鼠脑膜的结合(IC_50s:<1 uM)。胡椒基丁醚和(S)-甲基戊烯的效力较低(IC_50s:分别为21和63 uM)。与脾脏CB_2受体相比,苯并菲啶和胡椒基丁醚对脑CB_1受体的选择性更高。所有化合物均降低了[〜3H] SR141716A与CB_1受体结合的B_(max),但只有甲氧戊二烯和胡椒基丁醚会增加K_d(3-5倍)。苯并菲啶增加[〜3H] CP55940结合的K_d(6倍),但不改变B_(max)。 (S)-甲氧戊烯使[〜3H] CP55940结合的K_d增加了近4倍,B_(max)降低了60%。

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