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多巴胺对垂体前叶腺苷酸环化酶的抑制作用是通过D2受体的高亲和力状态介导的。

Dopamine inhibition of anterior pituitary adenylate cyclase is mediated through the high-affinity state of the D2 receptor.

作者信息

Borgundvaag B, George S R

出版信息

Life Sci. 1985 Jul 29;37(4):379-86. doi: 10.1016/0024-3205(85)90509-0.

DOI:10.1016/0024-3205(85)90509-0
PMID:4040201
Abstract

The diterpenoid forskolin stimulated adenylate cyclase activity (measured by conversion of [3H]-ATP to [3H]-cAMP) in anterior pituitary from male and female rats. Inhibition of stimulated adenylate cyclase activity by potent dopaminergic agonists was demonstrable only in female anterior pituitary. The inhibition of adenylate cyclase activity displayed a typically dopaminergic rank order of agonist potencies and could be completely reversed by a specific dopamine receptor antagonist. The IC50 values of dopamine agonist inhibition of adenylate cyclase activity correlated with equal molarity with the dissociation constant of the high-affinity dopamine agonist-detected receptor binding site and with the IC50 values for inhibition of prolactin secretion. These findings support the hypothesis that it is the high-affinity form of the D2 dopamine receptor in anterior pituitary which is responsible for mediating the dopaminergic function of attenuating adenylate cyclase activity.

摘要

二萜类化合物福斯高林可刺激雄性和雌性大鼠垂体前叶中的腺苷酸环化酶活性(通过将[3H]-ATP转化为[3H]-cAMP来测定)。强效多巴胺能激动剂对刺激的腺苷酸环化酶活性的抑制作用仅在雌性垂体前叶中得到证实。腺苷酸环化酶活性的抑制表现出典型的多巴胺能激动剂效力等级顺序,并且可以被特异性多巴胺受体拮抗剂完全逆转。多巴胺激动剂抑制腺苷酸环化酶活性的IC50值与高亲和力多巴胺激动剂检测到的受体结合位点的解离常数以及抑制催乳素分泌的IC50值呈等摩尔相关。这些发现支持了这样一种假说,即垂体前叶中D2多巴胺受体的高亲和力形式负责介导减弱腺苷酸环化酶活性的多巴胺能功能。

相似文献

1
Dopamine inhibition of anterior pituitary adenylate cyclase is mediated through the high-affinity state of the D2 receptor.多巴胺对垂体前叶腺苷酸环化酶的抑制作用是通过D2受体的高亲和力状态介导的。
Life Sci. 1985 Jul 29;37(4):379-86. doi: 10.1016/0024-3205(85)90509-0.
2
Dopaminergic inhibition of adenylate cyclase correlates with high affinity agonist binding to anterior pituitary D2 dopamine receptors.
Mol Cell Endocrinol. 1984 Jul;36(3):201-9. doi: 10.1016/0303-7207(84)90037-6.
3
Pharmacological characterization of the D2 dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary.大鼠垂体前叶中与腺苷酸环化酶负偶联的D2多巴胺受体的药理学特性
Mol Pharmacol. 1983 May;23(3):576-84.
4
Chronic estrogen treatment promotes a functional uncoupling of the D2 dopamine receptor in rat anterior pituitary gland.长期雌激素治疗可促进大鼠垂体前叶中D2多巴胺受体的功能解偶联。
Endocrinology. 1989 Jan;124(1):346-55. doi: 10.1210/endo-124-1-346.
5
Differential modulation of D1 and D2 dopamine-sensitive adenylate cyclases by 17 beta-estradiol in cultured striatal neurons and anterior pituitary cells.17β-雌二醇对培养的纹状体神经元和垂体前叶细胞中D1和D2多巴胺敏感性腺苷酸环化酶的差异调节作用。
J Neurochem. 1989 Feb;52(2):410-8. doi: 10.1111/j.1471-4159.1989.tb09136.x.
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Angiotensin II and dopamine modulate both cAMP and inositol phosphate productions in anterior pituitary cells. Involvement in prolactin secretion.
J Biol Chem. 1986 Mar 25;261(9):4071-5.
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Coupling of a cloned rat dopamine-D2 receptor to inhibition of adenylyl cyclase and prolactin secretion.克隆的大鼠多巴胺 D2 受体与腺苷酸环化酶抑制及催乳素分泌的偶联。
J Biol Chem. 1990 Feb 5;265(4):2098-104.
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Somatostatin inhibition of anterior pituitary adenylate cyclase activity: different sensitivity between male and female rats.
Brain Res. 1988 Jan 26;439(1-2):322-9. doi: 10.1016/0006-8993(88)91489-8.
9
Identification of a D1 dopamine receptor, not linked to adenylate cyclase, on lactotroph cells.在泌乳细胞上鉴定出一种与腺苷酸环化酶无关的D1多巴胺受体。
Br J Pharmacol. 1991 Aug;103(4):1928-34. doi: 10.1111/j.1476-5381.1991.tb12354.x.
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Multiple coupling of neurohormone receptors with cyclic AMP and inositol phosphate production in anterior pituitary cells.神经激素受体与垂体前叶细胞中环磷酸腺苷和肌醇磷酸生成的多重偶联。
Biochimie. 1987 Apr;69(4):271-9. doi: 10.1016/0300-9084(87)90017-4.

引用本文的文献

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Each individual isoform of the dopamine D2 receptor protects from lactotroph hyperplasia.多巴胺D2受体的每种单独亚型均可预防催乳素细胞增生。
Mol Endocrinol. 2013 Jun;27(6):953-65. doi: 10.1210/me.2013-1008. Epub 2013 Apr 22.
2
Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists.
Naunyn Schmiedebergs Arch Pharmacol. 1987 Nov;336(5):487-93. doi: 10.1007/BF00169304.
3
In vivo labelling of pituitary dopamine D-2 receptors in the male rat using [3H]-raclopride.使用[3H] - 雷氯必利对雄性大鼠垂体多巴胺D - 2受体进行体内标记。
J Neural Transm. 1989;76(1):13-28. doi: 10.1007/BF01244988.