Literature DB >> 6126877

Opiate antagonistic properties of an octapeptide somatostatin analog.

R Maurer, B H Gaehwiler, H H Buescher, R C Hill, D Roemer.   

Abstract

The somatostatin analog D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-NH-CH(CH2OH)CHOHCH3 (SMS 201-995) displaces [3h[naloxone from its binding sites (IC50, 38 +/- 60 nM), being more than 200 times more potent than somatostatin. As measured by the difference between [3H]dihydromorphine, [3H][D-Ala2,D-Leu5]enkephalin, and (-)-[3H]bremazocine binding, SMS 201-995 appears to be highly specific for the opiate mu binding site. Electrophysiological data from hippocampal cultures and results from animal studies (tail flick, mydriasis) demonstrate the opiate antagonistic properties of SMS 201-995. SMS 201-995 is an opiate mu antagonist with a peptide structure. That this property is displayed by a somatostatin analog is somewhat unexpected.

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Year:  1982        PMID： 6126877      PMCID： PMC346769          DOI： 10.1073/pnas.79.15.4815

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN： 0027-8424            Impact factor:   11.205


  18 in total

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  18 in total

1.  Tonic control of peripheral cutaneous nociceptors by somatostatin receptors.

Authors:  S M Carlton; J Du; S Zhou; R E Coggeshall
Journal:  J Neurosci       Date:  2001-06-01       Impact factor: 6.167

Review 2.  Mu opioids and their receptors: evolution of a concept.

Authors:  Gavril W Pasternak; Ying-Xian Pan
Journal:  Pharmacol Rev       Date:  2013-09-27       Impact factor: 25.468

Review 3.  Early engineering approaches to improve peptide developability and manufacturability.

Authors:  Jennifer L Furman; Mark Chiu; Michael J Hunter
Journal:  AAPS J       Date:  2014-10-23       Impact factor: 4.009

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Journal:  Biophys J       Date:  2001-02       Impact factor: 4.033

Review 5.  Design of peptide and peptidomimetic ligands with novel pharmacological activity profiles.

Authors:  Victor J Hruby; Minying Cai
Journal:  Annu Rev Pharmacol Toxicol       Date:  2013       Impact factor: 13.820

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Journal:  J Endocrinol Invest       Date:  1990-02       Impact factor: 4.256

7.  Tetrapeptide Endomorphin Analogs Require Both Full Length and Truncated Splice Variants of the Mu Opioid Receptor Gene Oprm1 for Analgesia.

Authors:  Gina F Marrone; Zhigang Lu; Grace Rossi; Ankita Narayan; Amanda Hunkele; Sarah Marx; Jin Xu; John Pintar; Susruta Majumdar; Ying-Xian Pan; Gavril W Pasternak
Journal:  ACS Chem Neurosci       Date:  2016-10-10       Impact factor: 4.418

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10.  Somatostatin- and enkephalin-like immunoreactivities are frequently colocalized in neurons in the caudal brain stem of rat.

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