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

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

  • Br J Pharmacol. 1993 Aug;109(4):898-9. doi: 10.1111/j.1476-5381.1993.tb13703.x.
J Dimech 1,  W Feniuk,  P P Humphrey
Affiliations

Affiliation

  • 1 Glaxo Institute of Applied Pharmacology, Department of Pharmacology, University of Cambridge.
PMID: 8104651 DOI: 10.1111/j.1476-5381.1993.tb13703.x
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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