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来自功能研究的进一步证据表明，豚鼠离体回肠、输精管和右心房存在生长抑素受体异质性。

Further evidence from functional studies for somatostatin receptor heterogeneity in guinea-pig isolated ileum, vas deferens and right atrium.

作者信息

Feniuk W, Dimech J, Jarvie E M, Humphrey P P

机构信息

Glaxo Institute of Applied Pharmacology, Department of Pharmacology, University of Cambridge.

出版信息

Br J Pharmacol. 1995 Jul;115(6):975-80. doi: 10.1111/j.1476-5381.1995.tb15906.x.

DOI:10.1111/j.1476-5381.1995.tb15906.x
PMID:7582529
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1909024/
Abstract
  1. Somatostatin (SRIF) causes a concentration-dependent inhibition of neurotransmission in guinea-pig ileum and vas deferens as well as negative inotropy in guinea-pig isolated right atrium. The SRIF receptors mediating these effects have now been further characterized by use of the peptides BIM-23027, BIM-23056 and L-362855, reported as selective for the recombinant SRIF receptor types, sst2, sst3 and sst5, respectively. 2. BIM-23027 was a highly potent agonist at causing an inhibition of neurotransmission in the guinea-pig ileum (EC50 value 1.9 nM), being about 3 times more potent than SRIF (EC50 value 6.8 nM). In contrast, in both guinea-pig vas deferens and right atrial preparations, BIM-23027 was a relatively weak agonist being at least 30-100 times weaker than SRIF. In guinea-pig atria, BIM-23027 (3 microM) antagonized the negative inotropic action of SRIF28 (apparent pKB = 5.9 +/- 0.1) but had no effect on the negative inotropic action of cyclohexyladenosine. 3. The inhibitory effect of BIM-23027 in the guinea-pig ileum was readily desensitized. Prior exposure to BIM-23027 (0.3 microM) markedly attenuated the inhibitory effect of SRIF but had no effect on the inhibitory action of clonidine suggesting that BIM-23027 and SRIF act via a common receptor mechanism. 4. L-362855 caused a concentration-dependent inhibition of neurotransmission in both the guinea-pig ileum and vas deferens as well as causing negative inotropy in the guinea-pig atrium but was at least 30-100 times weaker than SRIF. In guinea-pig isolated atria, L-362855 (3 microM) did not antagonize the negative inotropic action of SRIF28. 5. BIM-23056 in concentrations up to 1 microM was inactive as an agonist in guinea-pig isolated ileum, vas deferens and atrium and did not antagonize the inhibitory actions of SRIF in any of these preparations.6. The results from this study support our previous contention that the sst2 receptor type mediates inhibition of neurotransmission by SRIF in the guinea-pig ileum. The SRIF receptor type mediating inhibition of neurotransmission in the guinea-pig vas deferens appears different, but similar, to that mediating negative inotropy in the atrium. However the characteristics of these latter receptors appear different from that of the recombinant sst2, sst3 and sst5 receptors for SRIF described for rat and man.
摘要
  1. 生长抑素（SRIF）可使豚鼠回肠和输精管中的神经传递受到浓度依赖性抑制，并使豚鼠离体右心房出现负性肌力作用。介导这些效应的SRIF受体现已通过使用肽BIM - 23027、BIM - 23056和L - 362855进行了进一步表征，据报道这些肽分别对重组SRIF受体类型sst2、sst3和sst5具有选择性。2. BIM - 23027在抑制豚鼠回肠神经传递方面是一种高效激动剂（EC50值为1.9 nM），效力约为SRIF（EC50值为6.8 nM）的3倍。相比之下，在豚鼠输精管和右心房制剂中，BIM - 23027是一种相对较弱的激动剂，比SRIF至少弱30 - 100倍。在豚鼠心房中，BIM - 23027（3 microM）拮抗了SRIF28的负性肌力作用（表观pKB = 5.9±0.1），但对环己基腺苷的负性肌力作用无影响。3. BIM - 23027在豚鼠回肠中的抑制作用很容易脱敏。预先暴露于BIM - 23027（0.3 microM）可显著减弱SRIF的抑制作用，但对可乐定的抑制作用无影响，这表明BIM - 23027和SRIF通过共同的受体机制起作用。4. L - 362855可使豚鼠回肠和输精管中的神经传递受到浓度依赖性抑制，并使豚鼠心房出现负性肌力作用，但比SRIF至少弱30 - 100倍。在豚鼠离体心房中，L - 362855（3 microM）不拮抗SRIF28的负性肌力作用。5. 浓度高达1 microM的BIM - 23056在豚鼠离体回肠、输精管和心房中作为激动剂无活性，并且在这些制剂中均不拮抗SRIF的抑制作用。6. 本研究结果支持我们之前的观点，即sst2受体类型介导了SRIF对豚鼠回肠神经传递的抑制作用。介导豚鼠输精管神经传递抑制作用的SRIF受体类型似乎不同，但与介导心房负性肌力作用的受体类型相似。然而，后一种受体的特性似乎与大鼠和人类中描述的SRIF的重组sst2、sst3和sst5受体不同。

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本文引用的文献

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Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria.司美格鲁肽（MK 678）对豚鼠离体右心房生长抑素受体的拮抗作用。
Br J Pharmacol. 1993 Aug;109(4):898-9. doi: 10.1111/j.1476-5381.1993.tb13703.x.
2
Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.克隆的生长抑素受体：亚型选择性肽的鉴定及线性肽高亲和力结合的证明。
Mol Pharmacol. 1993 Jun;43(6):838-44.
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Characterization of cloned human somatostatin receptor SSTR5.克隆的人类生长抑素受体SSTR5的特性分析
Mol Pharmacol. 1994 Aug;46(2):291-8.
4
Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).肽类似物对所有五种克隆的人类生长抑素受体（hsstr 1 - 5）的亚型选择性。
Endocrinology. 1994 Dec;135(6):2814-7. doi: 10.1210/endo.135.6.7988476.
5
Characterization of somatostatin receptors in guinea-pig isolated ileum, vas deferens and right atrium.豚鼠离体回肠、输精管和右心房中生长抑素受体的特性研究
Br J Pharmacol. 1993 Nov;110(3):1156-64. doi: 10.1111/j.1476-5381.1993.tb13935.x.
6
Expression of multiple somatostatin receptor genes in AtT-20 cells. Evidence for a novel somatostatin-28 selective receptor subtype.多种生长抑素受体基因在AtT-20细胞中的表达。一种新型生长抑素-28选择性受体亚型的证据。
J Biol Chem. 1994 Jan 14;269(2):1506-9.
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Biochem Biophys Res Commun. 1993 Dec 15;197(2):366-71. doi: 10.1006/bbrc.1993.2488.
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