Benzthiazide

Benzthiazide是一种长效的利尿剂和抗高血压剂。Benzthiazide为碳酸酐酶9(carbonicanhydrase9(CA9))的抑制剂，对CA9，CA2和CA1的Ki值分别为8.0，8.8和10nM。Benzthiazide能够抑制肿瘤细胞增殖。

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Background

Benzthiazide is a long-acting diuretic[1] and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells[2].

Benzthiazide (0.4, 2, 10 μM) suppresses proliferation of cancer cell under hypoxic conditions in a dose-dependent manner. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively[2].

Benzthiazide (1, 1.5 mg/100 g BW) causes a marked decrease in urinary calcium excretion and the dissociation of calcium and sodium excretion in hyperprolactinemic rats[1].

[1]. Adler RA, et al. Hypercalciuria in hyperprolactinemic rats: effects of benzthiazide. Metabolism. 1986 Jul;35(7):668-72. [2]. Lee HS, et al. Rational drug repositioning guided by an integrated pharmacological network of protein, disease and drug. BMC Syst Biol. 2012 Jul 2;6:80.