Literature DB >> 8104651

Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria.

J Dimech1, W Feniuk, P P Humphrey.   

Abstract

Somatostatin (SS) exerts a negative inotropic effect in isolated atria. Here we report that in guinea-pig isolated right atria, seglitide, a potent cyclic hexapeptide somatostatin agonist, behaves as a competitive somatostatin receptor antagonist with pA2 values against SS14, SS25 and SS28, of 6.50 +/- 0.40, 6.24 +/- 0.08 and 6.09 +/- 0.06, respectively. Seglitide had little or no effect on the negative inotropic action of carbachol or N6-cyclohexyladenosine. Our findings indicate that the receptor-response coupling characteristics of guinea-pig atria are such that in this preparation seglitide has low intrinsic activity and behaves specifically as a somatostatin receptor antagonist.

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Year:  1993        PMID： 8104651      PMCID： PMC2175736          DOI： 10.1111/j.1476-5381.1993.tb13703.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  7 in total

1.  Subtypes of brain somatostatin receptors couple to multiple cellular effector systems.

Authors:  K Raynor; H L Wang; M Dichter; T Reisine
Journal:  Mol Pharmacol       Date:  1991-08       Impact factor: 4.436

Review 2.  Molecular biology of somatostatin receptors.

Authors:  G I Bell; T Reisine
Journal:  Trends Neurosci       Date:  1993-01       Impact factor: 13.837

3.  Subtypes of somatostatin receptors are expressed in the anterior pituitary cell line GH3.

Authors:  K Raynor; T Reisine
Journal:  J Pharmacol Exp Ther       Date:  1993-01       Impact factor: 4.030

4.  Some quantitative uses of drug antagonists.

Authors:  O ARUNLAKSHANA; H O SCHILD
Journal:  Br J Pharmacol Chemother       Date:  1959-03

5.  Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone.

Authors:  P Brazeau; W Vale; R Burgus; N Ling; M Butcher; J Rivier; R Guillemin
Journal:  Science       Date:  1973-01-05       Impact factor: 47.728

6.  A super active cyclic hexapeptide analog of somatostatin.

Authors:  D F Veber; R Saperstein; R F Nutt; R M Freidinger; S F Brady; P Curley; D S Perlow; W J Paleveda; C D Colton; A G Zacchei
Journal:  Life Sci       Date:  1984-04-02       Impact factor: 5.037

7.  An analysis of the negative inotropic action of somatostatin.

Authors:  R Quirion; D Regoli; F Rioux; S St-Pierre
Journal:  Br J Pharmacol       Date:  1979-06       Impact factor: 8.739
  7 in total
  4 in total

Review 1.  Molecular pharmacology of somatostatin receptors.

Authors:  D Hoyer; H Lübbert; C Bruns
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-11       Impact factor: 3.000

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

Authors:  W Feniuk; J Dimech; E M Jarvie; P P Humphrey
Journal:  Br J Pharmacol       Date:  1995-07       Impact factor: 8.739

3.  Mediation by SRIF1 receptors of the contractile action of somatostatin in rat isolated distal colon; studies using some novel SRIF analogues.

Authors:  E S McKeen; W Feniuk; P P Humphrey
Journal:  Br J Pharmacol       Date:  1994-10       Impact factor: 8.739

4.  Characterization of somatostatin receptors in guinea-pig isolated ileum, vas deferens and right atrium.

Authors:  W Feniuk; J Dimech; P P Humphrey
Journal:  Br J Pharmacol       Date:  1993-11       Impact factor: 8.739
  4 in total

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