Antagonist effects of seglitide (MK 678) at somatostatin receptors in guinea‐pig isolated right atria
Open Access
- 1 August 1993
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 109 (4) , 898-899
- https://doi.org/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.Keywords
This publication has 7 references indexed in Scilit:
- Molecular biology of somatostatin receptorsTrends in Neurosciences, 1993
- Subtypes of somatostatin receptors are expressed in the anterior pituitary cell line GH3.1993
- Subtypes of brain somatostatin receptors couple to multiple cellular effector systems.1991
- A super active cyclic hexapeptide analog of somatostatinLife Sciences, 1984
- AN ANALYSIS OF THE NEGATIVE INOTROPIC ACTION OF SOMATOSTATINBritish Journal of Pharmacology, 1979
- Hypothalamic Polypeptide That Inhibits the Secretion of Immunoreactive Pituitary Growth HormoneScience, 1973
- SOME QUANTITATIVE USES OF DRUG ANTAGONISTSBritish Journal of Pharmacology and Chemotherapy, 1959