Adenyl cyclase in human leukocytes: evidence for activation by separate beta adrenergic and prostaglandin receptors.
Adenyl cyclase in human leukocytes: evidence for activation by separate beta adrenergic and prostaglandin receptors.
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人类白细胞中的腺苷酸环化酶：通过单独的β肾上腺素能受体和前列腺素受体激活的证据。
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发表时间：
1971
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通讯作者：
K. Melmon
中科院分区：
文献类型：
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作者：
H. Bourne;K. Melmon
药物对离体人白细胞中腺苷酸环化酶活性的影响通过两种方法进行了检测：1）通过破碎细胞制备物将放射性三磷酸腺苷转化为环磷酸腺苷（AMP）; 2）用放射性腺嘌呤预孵育后，放射性环磷酸腺苷在完整白细胞中蓄积。环腺苷酸的合成增加，前列腺素E1（PGE 1）和选定的儿茶酚胺，但不是胰高血糖素或促肾上腺皮质激素。对儿茶酚胺的反应是β肾上腺素能受体的特征，无论是按照效力或激动剂的顺序[异丙肾上腺素=肾上腺素>去甲肾上腺素>苯肾上腺素（= 0）]，还是被β肾上腺素能拮抗剂（普萘洛尔和MJ-1999）竞争性抑制，但不被α拮抗剂（酚妥拉明和二苯那明）竞争性抑制。PGE 1的作用不被普萘洛尔阻断。PGE 1和异丙肾上腺素在最大有效剂量下对环AMP合成没有产生累加效应，表明这两种药物刺激不同的受体，但激活相同的腺苷酸环化酶。异丙肾上腺素的最大作用仅为PGE 1产生的作用的15%;异丙肾上腺素刺激一部分白细胞（或特定类型的白细胞）中腺苷酸环化酶的可能性尚未排除。
The effects of drugs on adenyl cyclase activity in isolated human leukocytes were examined in two ways: 1) conversion of radioactive adenosine triphosphate to cyclic adenosine monophosphate (AMP) by broken cell preparations; and 2) accumulation of radioactive cyclic AMP within intact leukoytes after preincubation with radioactive adenine. Synthesis of cyclic AMP was increased by prostaglandin-E1(PGE1) and selected catecholamines, but not by glucagon or adrenocorticotropin. Responses to catecholamines were characteristic of a beta adrenergic receptor, both in order of potency or agonists [isoproterenol = epinephrine > norepinephrine > phenylephrine (= 0)] and in being competitively inhibited by beta adrenergic antagonists (propranolol and MJ-1999) but not by alpha antagonists (phentolamine and Dibenamine). The effect of PGE1 was not blocked by propranolol. PGE1 and isoproterenol at maximally effective doses produced no additive effect on cyclic AMP synthesis, suggesting that both drugs stimulate different receptors, but activate the same adenyl cyclase enzyme. The maximum effect of isoproterenol is only about 15% of that produced by PGE1; the possibility that isoproterenol stimulates adenyl cyclase in a fraction of the leukocytes (or specific types of leukocytes) has not been ruled out.