L-36358

Seglitide acetate (MK-678 acetate) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide acetate also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS₁₄, SS₂₅ and SS₂₈, respectively. Seglitide acetate produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide acetate inhibits glucagon secretion and reduces circulating insulin levels. Seglitide acetate causes a sustained, reversible reduction in elevated systolic blood pressure in Streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide acetate induces membrane hyperpolarization and inhibits electrical excitability. Seglitide acetate induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide acetate can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus .