Abstract：
:The cyclic octapeptide, CYN-154806, inhibited specific [(125)I]-[Tyr(11)]-SRIF binding to CHO-K1 cell membranes expressing human recombinant somatostatin (SRIF) sst(2) receptors (pIC(50) 8. 58) or rat sst(2(a)) and rat sst(2(b)) receptors (pIC(50) 8.35 and 8. 10, respectively). The affinity of CYN-154806 at other human somatostatin receptor types was at least 100 times lower (pIC(50) 5. 41-6.48). In functional studies, CYN-154806 inhibited SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing h sst(2) receptors (pK(B) 7.92) but had no effect on UTP-induced increases in EAR. CYN-154806 also blocked SRIF-induced increases [(35)S]-GTPgammaS binding in CHO-K1 cell membranes expressing h sst(2) receptors as well as rat sst(2(a)) and rat sst(2(b)) receptors (pK(B) 7.81, 7.68 and 7.96, respectively). In marked contrast, no blockade was observed at h sst(5) receptors in concentrations as high 10 microM. The antagonistic activity of CYN-154806 was also studied in isolated tissue preparations that are known to express endogenous SRIF receptors. Thus CYN-154806 blocked SRIF, but not DAMGO-induced inhibition of neurogenic contractions in rat isolated vas deferens and guinea-pig ileum (pK(B) 7.79 and 7.49, respectively). CYN-154806 had no effect on SRIF-28 induced inhibition of neurogenic contractions in guinea-pig vas deferens. The results demonstrate that CYN-154806 is a highly potent specific and selective SRIF sst(2) receptor blocking drug. Furthermore, sst(2) receptors mediate SRIF-induced inhibition of neurogenic contractions in rat vas deferens and guinea-pig ileum but not guinea-pig vas deferens which is thought to be mediated by sst(5) receptors.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Feniuk W,Jarvie E,Luo J,Humphrey PPdoi
10.1016/s0028-3908(00)00035-6subject
Has Abstractpub_date
2000-06-08 00:00:00pages
1443-50issue
8eissn
0028-3908issn
1873-7064pii
S0028390800000356journal_volume
39pub_type
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更新日期：2014-01-01 00:00:00
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更新日期：2016-01-01 00:00:00
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pub_type： 杂志文章
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更新日期：1997-11-01 00:00:00
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pub_type： 杂志文章
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更新日期：2014-01-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：1982-05-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.06.003
更新日期：2013-12-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：1997-11-01 00:00:00
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pub_type： 杂志文章
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更新日期：2011-12-01 00:00:00
