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Tahara, A. et al.

Tahara, Tsukada, Tomura, Kusayama, Wada, Ishii, Yatsu, Uchida, Taniguchi, Tanaka,

Effect of YM471, an orally active non-peptide arginine vasopressin receptor antagonist, on human vascular smooth muscle cells.

OBJECTIVE: To investigate the effects of YM471, a non-peptide arginine vasopressin (AVP) V1A and V2 receptor antagonist, on the AVP-induced growth responses in human vascular smooth muscle cells (VSMCs). METHODS: Binding of YM471 to V1A receptors on VSMCs was measured using [3H]AVP. Intracellular free Ca2+ concentration was measured by fura 2 fluorescence. Mitogen-activated protein (MAP) kinase activity was determined using the p42/p44 MAP kinase specific peptide and [gamma- 32P]ATP as substrates. The effect of AVP on hyperplasia and hypertrophy of VSMCs was determined by cell number and protein content measurements. RESULTS: YM471 potently and concentration-dependently inhibited the specific binding of [ 3H]AVP to V1A receptors on VSMCs, exhibiting an inhibition constant (Ki ) of 0.35 nmol/l. YM471 inhibited the AVP-induced increase in intracellular free Ca concentration with an 50% inhibition concentration (IC50 ) of 2.01 nmol/l and inhibited the activation of MAP kinase with an IC50 of 6.11 nmol/l. In addition, AVP concentration-dependently induced hyperplasia and hypertrophy in VSMCs, but YM471 prevented these AVP-induced growth effects, exhibiting IC50 values of 2.31 and 0.23 nmol/l, respectively. CONCLUSIONS: These results indicate that YM471 has high affinity for V receptors on, and potently inhibits AVP-induced physiologic responses of, human VSMCs.[1]

References

Effect of YM471, an orally active non-peptide arginine vasopressin receptor antagonist, on human vascular smooth muscle cells. Tahara, A., Tsukada, J., Tomura, Y., Kusayama, T., Wada, K., Ishii, N., Yatsu, T., Uchida, W., Taniguchi, N., Tanaka, A. J. Hypertens. (2002) [Pubmed]

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