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

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The activity of peptides of the endothelin family in various mammalian smooth muscle preparations.

The activity of natural endothelins such as ET-1, ET-2, ET-3 and of sarafotoxin S6b (SRFTX) as compared to that of the C-terminal hexapeptide ET-(16-21) was investigated in several smooth muscle preparations in the presence of indomethacin, captopril, bestatin and thiorphan. In some tissues (rat thoracic aorta, guinea-pig ileum, human urinary bladder, renal pelvis or renal artery), ET-(16-21) had little if any agonist activity. In other preparations (guinea-pig bronchus, rat vas deferens, rabbit pulmonary artery) ET-(16-21) was a full agonist. The amidated form of ET-(16-21) was either inactive or less potent than ET-(16-21). These findings provide evidence that at least two receptors exist for peptides of the ET family; these receptors were termed ETA and ETB. ET-(16-21) is a full agonist at ETB receptors while being inactive or weakly active at ETA receptors. The free acid of tryptophan in position 21 plays a key role in the activity of these peptides at ETB receptors.[1]

References

  1. The activity of peptides of the endothelin family in various mammalian smooth muscle preparations. Maggi, C.A., Giuliani, S., Patacchini, R., Rovero, P., Giachetti, A., Meli, A. Eur. J. Pharmacol. (1989) [Pubmed]
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