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1. The relaxant effects of Zeneca ZD7114, BRL37344 (putative beta 3-adrenoceptor agonists) and various phenylethylamine-based agonists were studied in isolated ileum of the rat where tone was increased with carbachol (0.5 microM). Agonist-induced relaxation.was measured under equilibrium conditions with alpha-, beta 1- and beta 2-adrenoceptors inhibited. 2.(More)
1. Experiments were performed to characterize the effects of the novel brown adipocyte stimulant, ICI D7114, in the guinea-pig isolated ileum, right atrium and tracheal chain. In the ileum, agonist-induced inhibition of the contractile response to either histamine or prostaglandin E2 (PGE2) was assessed, along with effects on resting rate in the atrium and(More)
The endothelins (ET) are a group of proteins that act through G-protein coupled receptors. Endothelin-1 (ET-1) was initially identified as a potent vasoconstrictor and dysregulation of the ET axis contributes to pathological processes responsible for cardiovascular disease states. More recently, the ET axis, in particular ET-1 acting through the endothelin(More)
Endothelins are a family of small peptides (ET-1, ET-2, and ET-3) that mediate various physiological processes of mitogenesis, repair, and tissue differentiation by binding to endothelin A (ETA) and endothelin B (ETB) cell surface receptors. Activation of the ETA receptor by ET-1 has emerged as an important factor promoting tumor cell proliferation,(More)
Endothelin-1 is overexpressed in several tumor types. Activation of the endothelin-A (ETA) receptor may promote cell growth, angiogenesis and invasion, and inhibits the apoptotic process, while activation of the endothelin-B (ETB) receptor may induce cell death by apoptosis and inhibit tumor progression. Hypermethylation and subsequent silencing of the ETB(More)
The effects of substance P nonapeptide amide on inactivation of substance P by the guinea-pig ileum and urinary bladder preparations and of substance P hexapeptide amide, bradykinin and acetylcholine by the guinea-pig urinary bladder, have been investigated. Significant inhibition of inactivation of Substance P was found only in the urinary bladder. None of(More)
Rank order potency data for substance P (SP), physalaemin and eledoisin have been determined in a variety of assays in vitro. On the guinea-pig field stimulated vas deferens, physalaemin was approximately eight and five times more potent than eledoisin and SP respectively whereas in the rat field-stimulated vas deferens, eledoisin was approximately five(More)