Pharmacological Treatment of Benign Prostatic Hypertrophy

Caine, Marco

doi:10.1007/978-1-4471-1359-1_8

Cited by 2 publications

(1 citation statement)

References 17 publications

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“…In human prostate, Chapple et al (1991) suggested that the &JB subtype forms the majority of the a,-adrenoceptors, whereas Lepor et al (1993) and Testa et al (1993) using binding tests suggested that the dominant xl-adrenoceptor subtype in the human prostate is the O&1A subtype. Price et al (1993) investigated the mRNA expression of a,-adrenoceptors in the human prostate with specific probes for the a1A/D, a1B and mic subtypes, indicating that the predominant subtype is a&c. In addition to exogenous adrenergic stimulation, endogenous adrenergic stimulation plays an important role in human prostate since the tone of prostatic smooth muscle regulated by the autonomic nervous system is thought to be the 'dynamic' component of bladder outlet obstruction by BPH (Caine, 1986). Furthermore, a rather dense network of adrenergic nerve fibres has been found within the smooth muscle layer of the prostatic glandular stroma (Vaalasti & Hervonen, 1980).…”

Section: Introductionmentioning

confidence: 99%

Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

Guh

Chueh

et al. 1995

British J Pharmacology

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The effects of various α1‐adrenoceptor antagonists and nifedipine on tension responses of human prostate to electrical field stimulation were evaluated in this study. Prazosin (3 × 10−10 to 10−8M) and 5‐methyl‐urapidil (10−9 to 3 × 10−8 M) blocked concentration‐dependently the tension responses to electrical field stimulation and completely abolished them in the maximal concentrations (10−8 M and 3 × 10−8 M, respectively); in contrast, chloroethylclonidine (CEC), in the maximal concentration of 100 μM, blocked these effects by only 50%. The contractile responses of rat vas deferens and spleen to exogenously‐applied α1radrenoceptor agonists were competitively inhibited by prazosin and 5‐methyl‐urapidil; in addition, the pA2 values were calculated and the relative potencies with reference to prazosin were obtained. The relative potency of 5‐methyl‐urapidil in human prostate (0.105) was close to that in rat vas deferens (0.257), which contains primarily putative α1A‐adrenoceptors. However, it was much more than that in rat spleen (0.011), which contains primarily putative α1B‐adrenoceptors. Nifedipine (10−8 to 10−6 M) inhibited concentration‐dependently the contractile responses to electrical field stimulation in human prostate; in addition, the inhibition percentages were similar to those to exogenously‐applied noradrenaline in rat vas deferens. In contrast, CEC (10 μM), which almost flattened the concentration‐response curve of the rat spleen to phenylephrine, only partially inhibited (by 33.1%) the nerve‐mediated contraction of human prostate. The involvement of prejunctional α2‐adrenoceptors situated on the sympathetic nerve terminals of human prostate was also examined. Clonidine (3 × 10−9 to 3 × 10−7 M) blocked concentration‐dependently the contractile response to electrical field stimulation of human prostate and this inhibitory effect was reversed by yohimbine (10−7 M). Additionally, the inhibitory effect of CEC (3 × 10−6 to 3 × 10−4 M) to the nerve‐mediated contraction was also partially reversed by yohimbine (10−7M). It is suggested that the putative α1A‐adrenoceptors in human prostate may be functionally confined to the synaptic region whereas only minor populations of the putative α1B‐ and/or αlc‐adrenoceptors exist in this region.

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Section: Introductionmentioning

confidence: 99%

Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

Guh

Chueh

et al. 1995

British J Pharmacology

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In vitro and in vivo studies on the effects of the alpha‐adrenoceptor blocker IP/66 (1‐(2‐ethoxy‐2‐(3′ ‐pyridyl)ethyl)‐4‐(2′‐methoxy‐phenyl)piperazine) on urethral tone in rats

Manzini

Perretti

Boni

et al. 1991

Drug Development Research

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: In vitro and in vivo studies on the effects of the alpha-adrenoceptor blocker IPi66 (1 -(2-ethoxy-2-(3'-pyridyl)ethyl)-4-(2'-methoxy-phenyl)piperazine) on urethral tone in rats. Drug Dev. Res. 23: 35-46, 1991. IP/66 (1 -(2-ethoxy-2-(3'-pyridyl)ethyl)-4-(2'-methoxy-phenyl)piperazine is a newly synthetized and stereoselective alpha-adrenoceptor blocking drug. This compound exhibits preferential blocking activity in postjunctional as compared to prejunctional alpha-adrenergic responses. Furthermore, IP/66 inhibits phenylephrine-induced motor response in human and rat prostatic tissue and phenylephrine-, DMPP-and EFS-induced motor responses in rat urethral tissues, being equieffective or even more potent than prazosin. Like prazosin, intravenous administration of IP/66, at doses at which no hypotensive effect is observed, induces a marked inhibition of phenylephrine or DMPP-induced increase in urethral perfusion pressure, in anaesthetized pithed rats. Finally, IP/66 administration exerts beneficial effects in animals with surgically-or pharmacologically-induced urethral outflow obstruction. As a whole, the pharmacodynamic profile of IP/66 is promising and this drug might be proposed for clinical setting evaluating its efficacy for the treatment of lower urinary tract dysfunctions.

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Pharmacological Treatment of Benign Prostatic Hypertrophy

Cited by 2 publications

References 17 publications

Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

In vitro and in vivo studies on the effects of the alpha‐adrenoceptor blocker IP/66 (1‐(2‐ethoxy‐2‐(3′ ‐pyridyl)ethyl)‐4‐(2′‐methoxy‐phenyl)piperazine) on urethral tone in rats

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Pharmacological Treatment of Benign Prostatic Hypertrophy

Cited by 2 publications

References 17 publications

Characterization of α1‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

Characterization of α1‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

In vitro and in vivo studies on the effects of the alpha‐adrenoceptor blocker IP/66 (1‐(2‐ethoxy‐2‐(3′ ‐pyridyl)ethyl)‐4‐(2′‐methoxy‐phenyl)piperazine) on urethral tone in rats

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Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation

Characterization of α₁‐adrenoceptor subtypes in tension response of human prostate to electrical field stimulation