Khan M T, Wakade A R
Br J Pharmacol. 1979 Jun;66(2):223-8. doi: 10.1111/j.1476-5381.1979.tb13669.x.
1 The effect of guanethidine on the endogenous noradrenaline (NA) content, accumulation and overflow of [3H]-noradrenaline ([3H]-NA) in the rat salivary gland was examined at various times after drug administration. 2 Twenty-four h after a single injection of guanethidine (1 or 10 mg/kg s.c.), the respective values for the endogenous NA content and for the accumulation and overflow of [3H]-NA were approximately 55, 85, 30%, and 15, 55, 10% of the controls. 3 Although [3H]-NA accumulation had returned to control levels within 48 h after the dose of 10 mg/kg guanethidine, the overflow of [3H]-NA evoked by electrical stimulation or excess potassium (K+) remained depressed. 4 After the low or the high dose of guanethidine, the NA content of the salivary gland was restored to about 50% of the normal value between 4 to 24 and 48 to 72 h, respectively. 5 The accumulation of [3H]-NA was inhibited by about 75% by cocaine. The same degree of inhibition was obtained 4 h after 10 mg/kg guanethidine. In these experiments phenoxybenzamine did not reduce the residual (25%) uptake. 6 The reasons for differential rates of recovery of the endogenous NA content and the storage of [3H]-NA after guanethidine are discussed.
在给予胍乙啶后不同时间,检测了胍乙啶对大鼠唾液腺内源性去甲肾上腺素(NA)含量、[3H] - 去甲肾上腺素([3H] - NA)蓄积及溢出的影响。
单次皮下注射胍乙啶(1或10mg/kg)24小时后,内源性NA含量以及[3H] - NA的蓄积和溢出的相应值分别约为对照组的55%、85%、30%以及15%、55%、10%。
虽然给予10mg/kg胍乙啶剂量后48小时内[3H] - NA蓄积已恢复至对照水平,但电刺激或过量钾(K +)诱发的[3H] - NA溢出仍受抑制。
给予低剂量或高剂量胍乙啶后,唾液腺NA含量分别在4至24小时和48至72小时恢复至正常值的约50%。
可卡因使[3H] - NA的蓄积受到约75%的抑制。给予10mg/kg胍乙啶4小时后获得相同程度的抑制。在这些实验中,酚苄明并未降低残留的(25%)摄取。
讨论了胍乙啶后内源性NA含量和[3H] - NA储存恢复速率差异的原因。