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Chemical Compound Review:

CHEMBL34540 (3S)-3-[[(2S)-2-[[(2S)-2- amino-3-(3H...

Synonyms: SureCN7996606, CHEBI:153764, AC1L2VLI, ET-(16-21), 121377-67-1, ...

Douglas, S.A. et al., Miasiro, N. et al., Maggi, C.A. et al., Macchia, M. et al., Rovero, P. et al., et al.

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Psychiatry related information on His-leu-asp-ile-ile-trp

Effect of endothelin-1, endothelin-3 and C-terminal hexapeptide, endothelin (16-21) on motor activity in rats [1].

High impact information on His-leu-asp-ile-ile-trp

1. In the guinea-pig ileum the C-terminal hexapeptide of the endothelins, endothelin (16-21), induced a biphasic effect (relaxation followed by contraction) qualitatively similar to that seen in the responses to endothelins 1 and 3 [2].
3. Porcine proendothelin-1 had weak contractile activity in the isolated mesenteric bed but porcine endothelin (22-39), endothelin (16-21) and endothelin (16-21) amide did not have vasoconstrictor actions [3].
4. Endothelin-3, [Ala3,11]endothelin-1, [Ala1,3,11,15]endothelin-1 and endothelin (16-21) all had systemic blood pressure effects in the anaesthetized rat [3].
Endothelium-dependent mesenteric vasorelaxant effects and systemic actions of endothelin (16-21) and other endothelin-related peptides in the rat [3].
Vasorelaxation caused by endothelin (16-21) and its amide suggests that there is a receptor on the endothelium similar to one reported in the guinea-pig trachea.(ABSTRACT TRUNCATED AT 400 WORDS)[3]

Biological context of His-leu-asp-ile-ile-trp

1. We describe the results of a structure-activity study in which the C-terminal hexapeptide of the endothelins, endothelin (16-21), is compared with shorter fragments; hexapeptides bearing amino-acid substitutions and the corresponding C-terminal fragments of sarafotoxins [4].
3. Repeated administration of endothelin (16-21) induced no desensitization of the preparation, contrasting with the tachyphylaxis induced by endothelin-1 and endothelin-3 in the guinea-pig ileum [2].
Although endothelin (16-21) did not cause vasoconstriction in vitro, it increased mean arterial pressure in vivo but was at least 100 times less potent than endothelin-3 [3].
In an early report on the structure-activity relationship of endothelin (ET) peptides, it was reported that the C-terminal hexapeptide ET(16-21), His-Leu-Asp-Ile-Ile-Trp, is the minimum ET fragment which maintains biological activity in some, but not all the tissues responding to ETs [5].

Anatomical context of His-leu-asp-ile-ile-trp

In other preparations (guinea-pig bronchus, rat vas deferens, rabbit pulmonary artery) ET-(16-21) was a full agonist [6].
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 [6].
Binding characteristics of [125I]endothelin-1 in guinea-pig trachea and its displacement by endothelin-1, endothelin-3 and endothelin (16-21) [7].

Gene context of His-leu-asp-ile-ile-trp

Sarafotoxin S6c and the C-terminal hexapeptide endothelin (16-21) were inactive in these cells [8].
In the isolated rat urinary bladder ET-1, ET-3 and ET-(16-21) induced a dose-related contraction and a small enhancement of the neurogenic contraction caused by electrical field stimulation [9].
ET-(16-21) is a full agonist at ETB receptors while being inactive or weakly active at ETA receptors [6].

References

Effect of endothelin-1, endothelin-3 and C-terminal hexapeptide, endothelin (16-21) on motor activity in rats. Lecci, A., Maggi, C.A., Rovero, P., Giachetti, A., Meli, A. Neuropeptides (1990) [Pubmed]
Endothelin (16-21): biphasic effect and no desensitization on the guinea-pig isolated ileum. Miasiro, N., Nakaie, C.R., Paiva, A.C. Br. J. Pharmacol. (1993) [Pubmed]
Endothelium-dependent mesenteric vasorelaxant effects and systemic actions of endothelin (16-21) and other endothelin-related peptides in the rat. Douglas, S.A., Hiley, C.R. Br. J. Pharmacol. (1991) [Pubmed]
Structure-activity studies on endothelin (16-21), the C-terminal hexapeptide of the endothelins, in the guinea-pig bronchus. Rovero, P., Patacchini, R., Maggi, C.A. Br. J. Pharmacol. (1990) [Pubmed]
Toward the rational development of peptidomimetic analogs of the C-terminal endothelin hexapeptide: development of a theoretical model. Macchia, M., Barontini, S., Ceccarelli, F., Galoppini, C., Giusti, L., Hamdan, M., Lucacchini, A., Martinelli, A., Menchini, E., Mazzoni, M.R., Revoltella, R.P., Romagnoli, F., Rovero, P. Farmaco (1998) [Pubmed]
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]
Binding characteristics of [125I]endothelin-1 in guinea-pig trachea and its displacement by endothelin-1, endothelin-3 and endothelin (16-21). Tschirhart, E.J., Pelton, J.T., Jones, C.R. Agents Actions Suppl. (1990) [Pubmed]
BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cells. Hiley, C.R., Cowley, D.J., Pelton, J.T., Hargreaves, A.C. Biochem. Biophys. Res. Commun. (1992) [Pubmed]
Intracerebroventricular administration of endothelins: effects on the supraspinal micturition reflex and blood pressure in the anaesthetized rat. Lecci, A., Giuliani, S., Santicioli, P., Rovero, P., Maggi, C.A., Giachetti, A. Eur. J. Pharmacol. (1991) [Pubmed]

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