What question did this study set out to answer?

To evaluate and compare the in vitro vasoconstrictor activities and contractile potencies of porcine big endothelin-1, its truncated derivative, and mature 21-residue endothelin-1.

January 1, 1989Journal of Cardiovascular Pharmacology

Conversion of Big Endothelin-1 to 21-Residue Endothelin-1 Is Essential for Expression of Full Vasoconstrictor Activity

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Population

Porcine coronary artery strips (in vitro model)

Comparison

Synthetic big endothelin-1 [1-39] and big ET-1… vs 21-residue endothelin-1 (ET-1)

Design

Preclinical

Authors

SKSadao KimuraVascular / Pulmonary Vascular YKYoshitoshi KasuyaChiba University TSTatsuya SawamuraShinshu University

Discussion

Member takes

Implication

Big ET-1 precursors show lower coronary potency than ET-1; leaves open clinical relevance of ET converting enzyme inhibition in humans.

Key Points

To evaluate and compare the in vitro vasoconstrictor activities and contractile potencies of porcine big endothelin-1, its truncated derivative, and mature 21-residue endothelin-1.
Measured the contractile responses of isolated porcine coronary artery strips exposed in vitro to synthetic big ET-1 [1-39], big ET-1 [1-25], and mature 21-residue ET-1.
Synthetic big ET-1 [1-39] and big ET-1 [1-25] induced slow-developing, long-lasting, and strong vasoconstriction similar to 21-residue ET-1.
Contractile molar potencies of big ET-1 [1-39] and big ET-1 [1-25] were approximately 140-fold and 50-fold lower than that of mature ET-1, respectively.

Structured PICO

Population

Porcine coronary artery strips (in vitro model)

Intervention

Synthetic big endothelin-1 (big ET-1) [1-39] and big ET-1 [1-25]

Comparator

21-residue endothelin-1 (ET-1)

Outcome

Contraction of porcine coronary artery strips (vasoconstriction)surrogate

Conversion of big ET-1 to mature 21-residue ET-1 is essential for full vasoconstrictor activity, highlighting the physiological importance of ET converting enzyme.

Cite This Study

Kimura et al. (1989) studied this question.

synapsesocial.com/papers/6a898a211fb56efa37d458d4 https://doi.org/10.1097/00005344-198900135-00003

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Conversion of Big Endothelin-1 to 21-Residue Endothelin-1 Is Essential for Expression of Full Vasoconstrictor Activity

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

Conversion of Big Endothelin-1 to 21-Residue Endothelin-1 Is Essential for Expression of Full Vasoconstrictor Activity

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

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