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Chemical Compound Review:

Leu-thiorphan (2S)-2-[(2-benzyl-3- sulfanyl...

Synonyms: CTK3A6930, AC1L331I, 80970-04-3, 88728-48-7, Leucine thiorphan

Sekizawa, K. et al., Di Maria, G.U. et al., Kohrogi, H. et al., Kohrogi, H. et al.

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High impact information on Leucine thiorphan

Enkephalinase (120 micrograms) inhibited cough induced by subsequent exposure to substance P compared with the response to substance P alone, but after further exposure to the enkephalinase inhibitor leucine-thiorphan (10(-5) M), substance P increased cough significantly [1].
To study the roles of substance P and endogenous neutral endopeptidase in mediating cough, we measured cough responses in awake guinea pigs in response to exogenous substance P and capsaicin aerosols in the presence and absence of the neutral endopeptidase inhibitors leucine-thiorphan and phosphoramidon [2].
The addition of leucine-thiorphan to tracheal segments precontracted by 10(-9) and 10(-8) M endothelin-1 increased isometric tension by 181 +/- 65% (mean +/- 1 S.E.M.; P less than 0.05) and by 138 +/- 49% (P less than 0.05), respectively [3].
Leu-thiorphan shifted the dose-response curve to SP to lower concentrations [4].
Atropine or the SP antagonist [D-Pro2,D-Trp7,9]SP significantly inhibited SP-induced contractions in the presence of Leu-thiorphan [4].

Anatomical context of Leucine thiorphan

To determine the role of endogenous enkephalinase (EC 3.4.24.11) in regulating peptide-induced contraction of airway smooth muscle, we studied the effect of the enkephalinase inhibitor, leucine-thiorphan (Leu-thiorphan), on responses of isolated ferret tracheal smooth muscle segments to substance P (SP) and to electrical field stimulation (EFS) [4].

Gene context of Leucine thiorphan

The NEP inhibitor leucine-thiorphan (10(-5) M) significantly increased the contractile response to endothelin-1 [3].

References

Recombinant human enkephalinase (neutral endopeptidase) prevents cough induced by tachykinins in awake guinea pigs. Kohrogi, H., Nadel, J.A., Malfroy, B., Gorman, C., Bridenbaugh, R., Patton, J.S., Borson, D.B. J. Clin. Invest. (1989) [Pubmed]
Neutral endopeptidase inhibitors potentiate substance P- and capsaicin-induced cough in awake guinea pigs. Kohrogi, H., Graf, P.D., Sekizawa, K., Borson, D.B., Nadel, J.A. J. Clin. Invest. (1988) [Pubmed]
Neutral endopeptidase modulates endothelin-1-induced airway smooth muscle contraction in guinea-pig trachea. Di Maria, G.U., Katayama, M., Borson, D.B., Nadel, J.A. Regul. Pept. (1992) [Pubmed]
Enkephalinase inhibitor potentiates substance P- and electrically induced contraction in ferret trachea. Sekizawa, K., Tamaoki, J., Nadel, J.A., Borson, D.B. J. Appl. Physiol. (1987) [Pubmed]

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