References of "Pelton, J. T."
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See detailBinding characteristics of [125I]endothelin-1 in guinea-pig trachea and its displacement by endothelin-1, endothelin-3 and endothelin (16-21)
Tschirhart, Eric UL; Pelton, J. T.; Jones, C. R.

in Agents and Actions. Supplements (1991), 31

The presence of binding sites for endothelin-1 (ET-1) and endothelin-3 (ET-3) in airway epithelium, submucosa and smooth muscle of guinea-pig trachea was investigated using in vitro autoradiography. We ... [more ▼]

The presence of binding sites for endothelin-1 (ET-1) and endothelin-3 (ET-3) in airway epithelium, submucosa and smooth muscle of guinea-pig trachea was investigated using in vitro autoradiography. We also examined the ability of the C-terminal hexapeptide of endothelin, ET(16-21) to inhibit specific [125I]ET-1, binding. ET-1 appeared to bind to a single class of binding sites (nH not different from unity). In contrast, nH values for ET-3 displacement of [125I]ET-1 specific binding were different from unity, suggesting that these peptides bound to more than one site. ET (16-21) did not affect [125I]ET-1 binding. The present results suggest that the binding sites identified in guinea pig airway smooth muscle may be related to receptors mediating contractile responses to the endothelins. [less ▲]

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See detailEndothelins: functional and autoradiographic studies in guinea pig trachea
Tschirhart, Eric UL; Drijfhout, J. W.; Pelton, J. T. et al

in Journal of Pharmacology and Experimental Therapeutics (1991), 258(1), 381-7

The presence of binding sites for [125I]endothelin-1 and the contractile activities of endothelins (ETs) and sarafotoxin S6b and the endothelin fragment ET(16-21) were investigated in guinea pig trachea ... [more ▼]

The presence of binding sites for [125I]endothelin-1 and the contractile activities of endothelins (ETs) and sarafotoxin S6b and the endothelin fragment ET(16-21) were investigated in guinea pig trachea. ETs and sarafotoxin S6b (0.1-100 nM) induced potent contractile responses in guinea pig trachea with EC50 values ranging from 1.57 to 12.97 nM. Epithelium removal increased the potencies of ET-1, ET-2 and S6b, but not that of ET-3, and maximal responses to ET-1 and ET-2 were also increased. Effects of epithelium removal were partially mimicked by phosphoramidon (10 microM), an enkephalinase inhibitor, suggesting that enkephalinase (EC.3.4.24.11.) is able to degrade ET-1 and ET-2. ET-3-induced contractions were not affected by phosphoramidon. Autoradiographic studies suggested the presence of at least two specific binding sites for [125]ET-1 in guinea pig airway smooth muscle. The correlation between Kd and EC50 values suggests that the binding sites identified in the airway smooth muscle represent functional receptors for ETs. ET(16-21) and ET(16-21)-NH2 were less potent agonists than the ETs in guinea pig trachea and 10 microM ET(16-21) was unable to inhibit [125I]ET-1 binding in guinea pig airway smooth muscle. Therefore, these results suggest that the C-terminal hexapeptide of ET-1 cannot be used to classify ET receptors in guinea pig trachea. [less ▲]

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