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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

The pharmacological properties of the peptide, endothelin.

1. The effect of endothelin (ET-1) has been studied on isolated vascular and non-vascular preparations, using both functional and competition radioligand binding techniques. The effects of endothelin on blood pressure were studied in both anaesthetised, chemically denervated normotensive and spontaneously hypertensive rats (SHR). 2. Endothelin elicited contractile responses in the rat thoracic aorta, perfused mesenteric bed, rabbit mesenteric artery and portal vein. The maximal responses in the rat aorta were enhanced by removal of the endothelium, and were reduced in the presence of either a cyclo-oxygenase inhibitor (indomethacin) or a thromboxane receptor antagonist (SQ 29,548). In terms of potency, the most sensitive preparation was the rat endothelium-denuded aorta and rat perfused mesenteric bed (-log EC50 values = 8.2 +/- 0.07 and 8.2 +/- 0.12, mean +/- s.e.mean, n = 4, respectively). In the perfused mesenteric bed of the rat the maximum response to endothelin (219 +/- 12 mmHg, n = 4) was greater than that to either phenylephrine (maximal response = 67 +/- 9 mmHg; n = 4) or KCl (maximal response = 110 +/- 6 mmHg, n = 4). 3. Endothelin elicited contractile responses of the guinea-pig isolated ileum, oesophageal muscularis mucosae and uterus. Responses were also observed in the rat fundic strip and paced left atria. The guinea-pig urinary bladder, trachea, rat vas deferens and anococcygeus exhibited little or no response to endothelin at the concentrations studied (1 x 10(-12)-3.2 x 10(-8) M). Of the above preparations, the ileum and oesophageal muscularis mucosae were the most sensitive to endothelin (-log EC50 = 8.5 +/- 0.11 and 8.4 +/- 0.06, n = 6, respectively), exhibiting potencies similar to those observed in the endothelium-denuded aorta of the rat. 4. In competition-radioligand binding studies, endothelin did not displace either [3H]-PN 210-100 or [125I]-(-)-omega-conotoxin GVIA from binding sites in membranes from rat cerebral cortex and, skeletal muscle or from guinea-pig cerebral cortex and hippocampus, respectively. This indicates a lack of direct interaction of endothelin at the dihydropyridine binding site and the N-type calcium channel, respectively. However, in functional studies, contractile responses to endothelin (1 x 10(-8) M) in the endothelium-denuded aorta of the rat were potently reversed by nifedipine, verapamil, and prenylamine (-log IC50 values = 8.0 +/- 0.13, 7.2 +/- 0.09 and 6.6 +/- 0.08, n = 4-8, respectively).(ABSTRACT TRUNCATED AT 400 WORDS)[1]

References

  1. The pharmacological properties of the peptide, endothelin. Eglen, R.M., Michel, A.D., Sharif, N.A., Swank, S.R., Whiting, R.L. Br. J. Pharmacol. (1989) [Pubmed]
 
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