Evidence for a D1 dopamine receptor in the salivary glands of Amblyomma americanum (L.).

S P Schmidt, R C Essenberg, J R Sauer
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Abstract

Adenylate cyclase from the salivary gland of the lone star tick, Amblyomma americanum, is stimulated by several derivatives of phenylethylamine; dopamine, noradrenaline, adrenaline and isoproterenol. Octopamine and iota-DOPA had no effect on basal adenylate cyclase activity. Dopamine had the highest potency and the lowest Ka, 0.4 micron; followed by adrenaline and noradrenaline, 23 micron; and isoproterenol, 0.15mM. When either noradrenaline or adrenaline was added to dopamine, each at its maximally effective concentration, no additional stimulation of gland cyclase activity was noted. Furthermore, adrenaline and noradrenaline together did not equal the potency of dopamine alone. The most potent inhibitors of gland cyclase activity were the dopamine receptor antagonists. The phenothiazine drugs (thioridazine, chlorpromazine, and fluphenazine) were more effective inhibitors of cyclase activity than the butyrophenone drug (haloperidol). The inhibition constants (Ki) for the phenothiazine drugs were: 60nM for thioridazine, 1.9 micron for chlorpromazine and 2.3 micron for fluphenazine. The inhibition of adenylate cyclase activity was found to be specific for the (+) enantiomer of butaclamol, a stereospecific dopamine receptor antagonist. Our findings suggest that the lone star tick salivary gland adenylate cyclase has a D1 type dopamine receptor.

美洲钝瘤(Amblyomma americanum)唾液腺D1多巴胺受体的证据。
来自孤星蜱(Amblyomma americanum)唾液腺的腺苷酸环化酶被几种苯乙胺衍生物刺激;多巴胺,去甲肾上腺素,肾上腺素和异丙肾上腺素。章鱼胺和多巴对腺苷酸环化酶活性无影响。多巴胺效价最高,Ka最低,为0.4微米;其次是肾上腺素和去甲肾上腺素,23微米;异丙肾上腺素0.15mM。当去甲肾上腺素或肾上腺素分别以其最大有效浓度加入多巴胺时,没有注意到腺体环化酶活性的额外刺激。此外,肾上腺素和去甲肾上腺素一起作用并不等于单独使用多巴胺的效力。最有效的腺体环化酶活性抑制剂是多巴胺受体拮抗剂。吩噻嗪类药物(硫吡嗪、氯丙嗪和氟非那嗪)是比丁苯酮类药物(氟哌啶醇)更有效的环化酶活性抑制剂。对吩噻嗪类药物的抑制常数(Ki)分别为:噻嗪类60nM、氯丙嗪类1.9 nm、氟非那嗪类2.3 nm。腺苷酸环化酶活性的抑制作用对丁他卡莫(一种立体特异性多巴胺受体拮抗剂)的(+)对映体具有特异性。我们的研究结果表明,孤星蜱唾液腺腺苷酸环化酶具有D1型多巴胺受体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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