首页> 外国专利> USE OF 2,5-DIHYDROXYBENZOLSULPHONIC ACID DERIVATIVES IN THE PREPARATION OF A MEDICAMENT FOR INCREASING THE EFFECT OF OTHER MEDICAMENTS FOR TREATING THE EFFECTIVE DYSFUNCTION

USE OF 2,5-DIHYDROXYBENZOLSULPHONIC ACID DERIVATIVES IN THE PREPARATION OF A MEDICAMENT FOR INCREASING THE EFFECT OF OTHER MEDICAMENTS FOR TREATING THE EFFECTIVE DYSFUNCTION

机译:2,5-二羟基苯磺酸硫代酸衍生物在制备药物中的用途,以增强其他药物对有效功能障碍的治疗作用

摘要

Use of 2,5-dihydroxy-benzenesulfonic (or 1,4-disulfonic) acid calcium or diethylammonium salts (I) for potentiating the effect of agents (II) for stimulating penile erection in humans. Use of 2,5-dihydroxy-benzenesulfonic acid derivatives of formula (I) in the production of a medicament for potentiating the effect of agents (II) for stimulating penile erection in humans, where (II) are selected from phosphodiesterase V inhibitors, apomorphine, nitrogen monoxide donors, agents for increasing cyclic guanosine monophosphate (cGMP) levels in penile tissue and other agents for this purpose. [Image] R : H or DSO 3 -; A : Ca 2 + or N +H 2Et 2; and n, m : 1 or 2. ACTIVITY : Vasotropic. In isolated human corpus cavernosum, calcium dobesilate (Ia) at a concentration of 10 mu M significantly increased the relaxation of resistant arteries produced by specific concentrations of the phosphodiesterase inhibitor sildenafil (IIa). The relaxation was ca. 25% in presence of 10 nM (IIa) alone and ca. 65% in presence of 10 nM (IIa) and 10 mu M (Ia). MECHANISM OF ACTION : Promotion of relaxation of resistant arteries in the penis.
机译:2,5-二羟基苯磺酸(或1,4-二磺酸)酸钙盐或二乙铵盐(Ⅰ)用于增强药剂(Ⅱ)刺激人类阴茎勃起的作用。式(I)的2,5-二羟基苯磺酸衍生物在制备药物中的用途,所述药物用于增强试剂(II)对人的阴茎勃起的刺激作用,其中(II)选自磷酸二酯酶V抑制剂阿扑吗啡,一氧化氮供体,用于增加阴茎组织中环鸟苷单磷酸(cGMP)水平的试剂和其他用于此目的的试剂。 [图片] R:H或DSO 3->; A:Ca 2> +>或N +> H 2Et 2; n,m:1或2。活性:垂直。在分离的人海绵体中,浓度为10μM的苯磺酸硅酸钙(Ia)显着增加了特定浓度的磷酸二酯酶抑制剂西地那非(IIa)产生的抗性动脉的舒张。放松是大约。 25%在单独存在10 nM(IIa)和65%存在10 nM(IIa)和10μM(Ia)。作用机理:促进阴茎中抵抗性动脉的松弛。

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