Two types of somatostatin receptors differentiated by cyclic somatostatin analogs.

Two types of somatostatin receptors differentiated by cyclic somatostatin analogs.
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通过环状生长抑素类似物区分两种类型的生长抑素受体。

DOI:
10.1126/science.2858917
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发表时间:
1985
期刊:
Science (New York, N.Y.)
影响因子:
--
通讯作者:
Martin,JB
Martin,JB
中科院分区:
--
文献类型:
--
作者:
Tran,VT;Beal,MF;Martin,JB

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用生长抑素14和28的两种放射性碘标记类似物标记大鼠脑、垂体和胰腺中的生长抑素受体。生长抑素的两个环状类似物,SMS 201 -995和cyclo(Ala-Cys-Phe-D-Trp-Lys-Thr-Cys),显示通过这些放射性配体与生长抑素受体结合的双相置换。相反,所有其他生长抑素类似物,包括生长抑素-14,竞争的受体位点的放射性配体受体结合的双相位移。因此,确定了两种类型的生长抑素受体。研究发现,垂体和胰腺主要有一种类型的生长抑素受体,而大脑有两种,大脑的不同区域有不同比例的两种类型。这些研究结果表明,方法来表征其他类型的生长抑素受体subserving生长抑素的各种生理功能,包括在认知功能和锥体外系运动系统控制的潜在作用。
Somatostatin receptors in rat brain, pituitary, and pancreas were labeled with two radioiodinated analogs of somatostatins 14 and 28. Two cyclic analogs of somatostatin, SMS201-995 and cyclo(Ala-Cys-Phe-D-Trp-Lys-Thr-Cys), showed biphasic displacement of binding to somatostatin receptors by these radioligands. In contrast, all other somatostatin analogs, including somatostatin-14, competed for the receptor sites with monophasic displacement of radioligand receptor binding. Thus two types of somatostatin receptors were identified. It was found that the pituitary and pancreas have predominantly one type of somatostatin receptor whereas the brain has both, and that different regions of the brain have various proportions of the two types. These findings suggest methods to characterize other types of somatostatin receptors subserving somatostatin's diverse physiological functions, including a potential role in cognitive function and extrapyramidal motor system control.
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