Disease relevance of YM-12617

• In the present study a newly synthesized alpha 1-blocker, YM-12617, was tried and evaluated in 77 male patients with mild benign prostatic hyperplasia and in 5 women with micturition difficulties of unknown origin [1].

High impact information on YM-12617

• Electrical and mechanical properties of the capsular smooth muscles of the rabbit prostate in relation to the actions of the alpha 1-adrenoceptor blocker, YM-12617 [2].
• The affinities of prazosin and YM-12617 compounds for [3H]prazosin binding sites in hypertrophied prostates of humans correlated closely with their pharmacological potencies in prostates reported previously [3].
• Alpha-1 adrenoceptor antagonist effects of the optical isomers of YM-12617 in rabbit lower urinary tract and prostate [4].
• The alpha-1 selective antagonists YM 12617 and WB 4101 blocked the inhibitory action of NE with IC50 values of about 0.1 and 1 nM, respectively, whereas the alpha-2 selective antagonists Wy 26703 and rauwolscine were much less potent [5].
• The effects of YM-12617 on the electrophysiological properties of smooth muscle membranes and prejunctional nerve terminals and contractions evoked by different procedures were studied using guinea-pig mesenteric and pulmonary arteries [6].

Biological context of YM-12617

• When YM-12617, in concentrations over 1 microM, was applied to the mesenteric artery the amplitude of the first excitatory junction potential evoked by a train stimulation of perivascular nerves was inhibited, but the facilitation of excitatory junction potentials evoked by frequencies over 0.1 Hz was enhanced [6].
• Among the desoxy derivatives, YM-12617 was more potent than prazosin in blocking alpha 1-adrenoceptors in anaesthetized rats and in reducing blood pressure, total peripheral resistance and left ventricular work in anaesthetized dogs [7].

Anatomical context of YM-12617

• Effects of YM-12617, an alpha adrenoceptor blocking agent, on electrical and mechanical properties of the guinea-pig mesenteric and pulmonary arteries [6].
• These results suggest that YM-12617 is capable of protecting the myocardium from hypoxia-induced disturbances of cardiac function and metabolism [8].
• Although YM-12617 was also a competitive antagonist toward clonidine at prejunctional alpha 2-adrenoceptors in the isolated rat vas deferens, its affinity for these receptors (pA2 = 6.41) was 5,000 times lower than that displayed for the postjunctional alpha 1-adrenoceptors in the isolated rabbit aorta [9].
• The curves of norepinephrine and phenylephrine were also shifted by YM-12617 in the portal vein, where the efficacies of both the alpha 1-agonists were high [10].

Associations of YM-12617 with other chemical compounds

• The alpha-1 adrenoceptor antagonist effects of the optical isomers of YM-12617 (5-[2-[[2-(o-ethoxyphenoxy)ethyl]amino]propyl]- 2-methoxybenzenesulfonamide HCl), a potent and selective alpha-1 adrenoceptor antagonist, were evaluated in the rabbit lower urinary tract and prostate [4].

Gene context of YM-12617

• Use of an alpha 1-blocker, YM-12617, in micturition difficulty [1].

Analytical, diagnostic and therapeutic context of YM-12617

• 1. Electrical and mechanical properties of smooth muscle cells of the rabbit prostate capsule and the actions of the alpha 1-adrenoceptor blocker, YM-12617, were investigated using microelectrode and isometric tension recording methods [2].
• Isolated rabbit hearts were perfused for 25 min under hypoxic conditions in the absence or the presence of 28 microM YM-12617, followed by 45 min with oxygenated perfusion medium, and functional and metabolic changes of the heart were examined [8].
• Sensitive method for the determination of amsulosin in human plasma using high-performance liquid chromatography with fluorescence detection [11].

References