Coates J, Weetman D F
Br J Pharmacol. 1983 Oct;80(2):343-6. doi: 10.1111/j.1476-5381.1983.tb10039.x.
Sgd 101/75 (4(2-imidazoline-amino)-2-methylindazol-chlorhydrate) and noradrenaline exerted similar, full agonist effects on the alpha-adrenoceptors of the rat anococcygeus. Benextramine (30 microM for 30 min, followed by 20 washes over 30 min) abolished contractions of the anococcygeus to Sgd 101/75, but only reduced those to noradrenaline. Sgd 101/75 (400 microM) did not significantly reduce contractions of the benextramine-treated (30 microM) anococcygeus to noradrenaline. It is concluded that benextramine can replace phenoxybenzamine as the alkylating agent in the demonstration of alpha 1s-adrenoceptors in the rat anococcygeus.
Sgd 101/75(4-(2-咪唑啉氨基)-2-甲基吲唑盐酸盐)和去甲肾上腺素对大鼠肛尾肌的α-肾上腺素能受体产生相似的完全激动剂作用。苄非他明(30微摩尔,作用30分钟,随后在30分钟内冲洗20次)消除了肛尾肌对Sgd 101/75的收缩反应,但仅减弱了对去甲肾上腺素的收缩反应。Sgd 101/75(400微摩尔)并未显著减弱经苄非他明(30微摩尔)处理的肛尾肌对去甲肾上腺素的收缩反应。得出的结论是,在大鼠肛尾肌α1s-肾上腺素能受体的证明中,苄非他明可替代酚苄明作为烷基化剂。