Drotaverine hydrochloride 是磷酸二酯酶 4 (PDE4)的抑制剂,也是L 型电压依赖钙通道(L-VDCC)的阻滞剂,可阻断3',5'-环腺苷单磷酸的降解。它在体内有抗痉挛效果,但无抗胆碱能的效果。
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描述
Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine
体外活性
drotaverine not only relaxed the precontracted tracheal preparations but also decreased mediator-induced contraction.?These effects of drotaverine were concentration dependent, with a significantly higher potency on the KCl-induced response, than on either the histamine or methacholine induced one.?A similar result was noted for nifedipine.?The PDE inhibitor, theophylline, also relaxed the precontracted preparations but was ineffective on the mediator-induced contraction in a physiologically relevant concentration range.
Cas No.
985-12-6
分子式
C24H32ClNO4
分子量
433.97
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years