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  • Title: Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea-pig isolated right atria.
    Author: Dimech J, Feniuk W, Humphrey PP.
    Journal: Br J Pharmacol; 1993 Aug; 109(4):898-9. PubMed ID: 8104651.
    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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