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The effects of synthetic analogs of sarafotoxin (STX) S6b, a snake venom peptide with a high sequence homology to the endothelium-derived vasoconstrictor endothelin (ET), on ET receptor binding activity and cytosolic free Ca2+ concentration [( Ca2+]i) were studied in cultured rat vascular smooth muscle cells. Binding studies revealed that [Cys1-15, Cys3-11] STX competed with 125I-ET for the binding to its vascular receptors with lower affinity than that of ET, but was far more effective than [Cys1-11, Cys3-15]STX in inhibiting the binding. [Cys1-15, Cys3-11]STX had a less potent effect on increasing [Ca2+]i than ET, whereas [Cys1-11, Cys3-15]STX was inactive. These data suggest that there may exist heterogenous subpopulations of the vascular ET/STX receptors, and that the proper double cyclic structure of STX is essential for interacting with its putative receptors to induce the [Ca2+]i response.
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
August 1989,
Biochemical and biophysical research communications,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
September 1989,
Biochemical and biophysical research communications,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
October 1989,
European journal of pharmacology,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
January 1990,
Life sciences,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
March 1992,
British journal of pharmacology,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
January 1989,
Biochemical and biophysical research communications,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
January 1992,
Glia,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
January 1992,
Life sciences,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
January 1991,
Neurochemistry international,
Y Hirata, and
H Yoshimi, and
F Marumo, and
T X Watanabe, and
S Kumagaye, and
K Nakajima, and
T Kimura, and
S Sakakibara
August 1993,
European journal of pharmacology,
