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YM-430, also known as YM-15430; YM-154301; is a dual of β1 adrenergic receptor antagonist and calcium channel antagonist. YM430 could be both an antianginal and antihypertensive agent, because of its dual activities. YM430 (10(-8)-10(-6) M) inhibited 3,4-diaminopyridine-induced rhythmic contractions with an IC50 value of 59.2 nM. In anesthetized rats, YM430 (10-100 mg/kg PO) inhibited arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg PO. YM430 may be of value in the treatment of various types of angina pectoris such as variant and stable angina. | [Uses]
YM-430 is an oral active calcium entry-blocking and beta-adrenoceptor-blocking agent. YM-430 inhibits Amifampridine (HY-14946)-induced rhythmic contractions with an IC50 value of 59.2 nM and inhibits arginine vasopressin-induced ST-segment depression with an IC50 value of 36.6 mg/kg. YM-430 can be used for study of angina pectoris[1]. | [References]
[1] Shibasaki K, et al. Antianginal effects of YM430, a novel calcium entry-blocking and beta-adrenoceptor-blocking agent in several experimental angina models. Gen Pharmacol. 1997;29(4):545-550. DOI:10.1016/s0306-3623(96)00567-8 |
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CHEMICAL LAND21
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www.chemicalland21.com |
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