Reference

Alpha-1 adrenoceptor antagonist effects of the optical isomers of YM-12617 in rabbit lower urinary tract and prostate

Alpha-1 adrenoceptor antagonist effects of the optical isomers of YM-12617 in rabbit lower urinary tract and prostate. Honda, Kazuo; Nakagawa, Chieko (Cent. Res. Lab., Yamanouchi Pharm. Co., Ltd., Tokyo 174, Japan). J. Pharmacol. Exp. Ther., 239(2), 512-16 (English) 1986. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The a1-adrenoceptor antagonist effects of the optical isomers of YM-12617 (I), a potent and selective a1-adrenoceptor antagonist, were evaluated in the rabbit lower urinary tract and prostate. (R-(-)-YM-12617 [106133-20-4] (1 ′ 10-10-3 ′ 10-9M) and S-(+)-YM-12617 [106138-88-9] (3 ′ 10-8-3 ′ 10-7M) antagonized phenylephrine-induced contraction in a competitive manner in the urinary bladder base (trigone), proximal urethra and prostate. The mean pA2 value for R-(-)-YM-12617 at the a1-adrenoceptor of trigone, urethra, and prostate was 9.91, 9.62 and 9. 106138-88-9 and 10-10-3 are also in the experiment.92, resp., and that for S-(+)-YM-12617 was 8.09, 7.92, and 7.77, resp. Therefore, R-(-)-YM-12617 is a 50-141-fold more potent antagonist than S-(+)-YM-12617 at the a1-adrenoceptor in these tissues. The results also indicate that the a1-adrenoceptor in the lower urinary tract and prostate can distinguish clearly between the optical isomers of YM-12617. Similar results were obtained in the aorta of rabbits, in which a dramatic stereochem. preference of R-(-)-YM-12617 for the a1-adrenoceptor also exists. .

Tamsulosin and chlormadinone for the treatment of benign prostatic hyperplasia

Tamsulosin and chlormadinone for the treatment of benign prostatic hyperplasia. Okada, Hiroshi; Kawaida, Noriyuki; Ogawa, Takayoshi; Arakawa, Soichi; Matsumoto, Osamu; Kamidono, Sadao; et al. (Dep, Urol., Kobe Univ. Sch. Med., Kobe, Japan). Scandinavian Journal of Urology and Nephrology, 30(5), 379-385 (English) 1996 Scandinavian University Press. CODEN: SJUNAS. ISSN: 0036-5599. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The recent introduction of selective a-adrenoceptor blockers adds a further therapeutic option for the treatment of benign prostatic hyperplasia (BPH). Tamsulosin, a selective a1-blocker, has proved effective in relieving irritative and obstructive symptoms caused by BPH. To investigate whether the combination of tamsulosin with the anti-androgenic drug chlormadinone is of further therapeutic benefit, 80 patients randomly received tamsulosin 0.2 mg daily, chlormadinone 50 mg daily or combination of tamsulosin 0.2 mg and chlormadinone 50 mg daily for 16 wk. Greater improvement in subjective symptoms of BPH was obtained with with er tamsulosin alone or in combination with chlormadinone than with chlormadinone alone. However, the greatest improvement in objective uroflowmetric data was obtained with chlormadinone in combination with tamsulosin. Thus, the combination of tamsulosin with chlormadinone appears to be more beneficial than either of these agents used as monotherapy. Further investigation is required to fully evaluate the therapeutic effects of this combination. 1961-77-9 and 106133-20-4 which are cas registry numbers of substances are two of reagents here. After the trial period one-third of the chlormadinone and tamsulosin/chlormadinone-treated patients needed no further treatment due to the satisfactory relief of symptoms. At 12 mo follow-up, however, one-fourth of the patients had undergone transurethral resection of the prostate (TUR-P) regardless of medication. This suggests a limitation of the medical treatment of BPH. .