Garnovskaia M N, Tret'iakov A V, Maslova M N, Etingof R N
Ukr Biokhim Zh (1978). 1990 Jan-Feb;62(1):97-101.
It is shown, that p-aminobenzoic acid and its derivatives (p-acetylaminobenzoic acid and p-aminobenzoic acid hydrazide) in the concentration of 10(-6) M are the potent inhibitors (40% below the control specimens) of the phosphodiesterase activity of cyclic nucleotides in the soluble fraction of the adult rat uterus. These drugs exerted no action on the adenylate cyclase activity in membrane fractions. The inhibition is only specific to the uterus enzyme and is not revealed for other tissues. The inhibition is found to be of incompetitive character Ki for p-aminobenzoic acid hidrazide being equal to 3.2 microM.
结果表明,对氨基苯甲酸及其衍生物(对乙酰氨基苯甲酸和对氨基苯甲酰肼)在浓度为10⁻⁶ M时,是成年大鼠子宫可溶性部分中环状核苷酸磷酸二酯酶活性的强效抑制剂(比对照标本低40%)。这些药物对膜部分中的腺苷酸环化酶活性没有作用。这种抑制作用仅对子宫酶具有特异性,在其他组织中未观察到。发现这种抑制作用具有非竞争性特征,对氨基苯甲酰肼的Ki等于3.2微摩尔。