Comparison of the gastric exocrine inhibitory activities and plasma kinetics of somatostatin-28 and somatostatin-14 in cats

The gastric exocrine inhibitory activities of somatostatin-28 (SS-28) and somatostatin-14 (SS-14) were determined in conscious cats prepared with gastric fistulae. Gastric acid and pepsin secretions were stimulated with pentagastrin. Expressed in terms of exogenous doses, SS-14 (ID 50: 1.49 nmol · k...

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Veröffentlicht in:Regulatory peptides 1982-09, Vol.4 (4), p.227-237
Hauptverfasser: Hirst, Barry H., Conlon, J.Michael, Coy, David H., Holland, Joy, Shaw, Bernard
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Sprache:eng
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Zusammenfassung:The gastric exocrine inhibitory activities of somatostatin-28 (SS-28) and somatostatin-14 (SS-14) were determined in conscious cats prepared with gastric fistulae. Gastric acid and pepsin secretions were stimulated with pentagastrin. Expressed in terms of exogenous doses, SS-14 (ID 50: 1.49 nmol · kg −1 · h −1) was 3.4 times more potent than SS-28 (ID 50: 5.12 nmol · kg −1 · h −1) as an inhibitor of gastric acid secretion. Similarly SS-14 (ID 50: 0.25 nmol · kg −1 · h −1) was 3.8 times more potent than SS-28 (ID 50: 0.96 nmol · kg −1 · h −1) as an inhibitor of pepsin secretion. Expressed in terms of circulating plasma concentration measured by radioimmunoassay, SS-14 (ID 50: H +, 232 and pepsin 73 pM) was 8–9 times more potent than SS-28 (ID 50: H +, 2112 and pepsin, 611 pM) as an inhibitor of gastric exocrine secretions. The plasma immunoreactive half-life of SS-28 (6.1 min) was double that for SS-14 (2.4 min) possibly due to a slower theoretical metabolic clearance rate of the larger peptide (30 and 87 ml · kg −1 · min −1, respectively). Both peptides had similar apparent distribution volumes (SS-14, 306 and SS-28, 263 ml · kg −1). As judged by gel chromatography of plasma samples, there was no evidence for the conversion of SS-28 to SS-14 in vivo. The reduced activity of SS-28, compared with SS-14, against gastric exocrine secretions contrasts with its more potent effects in the pituitary and pancreas.
ISSN:0167-0115
1873-1686
DOI:10.1016/0167-0115(82)90115-X