Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-03-17
1998-05-12
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514397, A61K 3144, A61K 31415
Patent
active
057505373
DESCRIPTION:
BRIEF SUMMARY
This Application is a 371 of PCT/JP95/01745 filed Aug. 31, 1995.
TECHNICAL FIELD
The present invention relates to a therapeutic agent for impotence which comprises a 5HT.sub.3 antagonist as the active ingredient, and is useful in the medical field.
BACKGROUND ART
5HT receptors are classified into the subtypes of 5HT.sub.1, 5HT.sub.2, 5HT.sub.3, 5HT.sub.4, 5HT.sub.5, 5HT.sub.6 and 5HT.sub.7 (see D. Hoyer et al., Pharmacol. Rev., 1994 in press; P.P.A. Humphrey et al., Trends Pharmacol. Sci., 14, 233, 1993).
It is reported that 5HT1 receptors are densely distributed in smooth muscle, cerebral cortex, hippocampus, ventral horn of spinal cord, basal ganglia, etc., and are involved in the depression of nervous system and in the modulation of cardiovascular system (e.g., hypotension, tachycardia, dilation and contraction of vascular smooth muscle) and so on;
that 5HT.sub.2 receptors are densely distributed in smooth muscle, motor cortex, etc., and are involved in the depolarization of motor nerve, modulation of body temperature, hypertension, vasoconstriction and the contraction of smooth muscle in digestive tract, trachea and vesica; and
that 5HT.sub.3 receptors are densely distributed in both peripheral and central nervous system including human cerebral cortex, etc., and are involved in the expression of emesis and the attack of hemicrania (see A.H Dickenson's review on 5HT).
Recently, the need for a therapeutic agent for impotence has been growing clinically. Although there is a therapeutic method for impotence in which vasoactive drugs such as papaverine or PGE1 are injected directly in corpus cavernosum, this method is not desirable because of some undesirable side effects or the methodology. Consequently, the development of an effective oral therapeutic agent for impotence has been needed. Up to the present, however, the effects of conventional oral drugs which were considered to be beneficial for impotence has been proved to be unsatisfactory, because of their poor efficacy, their safety, or undesirable side effects.
It has been reported that 5HT (serotonin) is involved in the expression of sexual behavior (see Gessa GL, Tangliamonte A, In Sexual Behavior, Pharmacology and Biochemistry, edited by Sandler Mand, Gessa GL, New York; Raven Press, 1975). On the other hand, regarding the relationship between 5HT.sub.3 receptors and sexual behavior, it is reported that 5HT.sub.3 antagonist had no effect on sexual behavior in normal (non-stressed) animals (see Stoessl AJ et al., Brain Res. 517, 111, 1990; Tanco SA et al., Experimentia 49, 238, 1991).
The object of the present invention is to provide a novel and effective medicine for the treatment of impotence.
DISCLOSURE OF THE INVENTION
We, the inventors of the present invention, found that a 5HT.sub.3 antagonist is effective for the treatment of impotence, and have completed the present invention on the basis of this finding.
Specifically, the present invention relates to a therapeutic agent for impotence which comprises a 5HT.sub.3 antagonist as an active ingredient.
The 5HT.sub.3 antagonist as referred to this invention includes a drug having a stronger antagonistic effect against 5HT.sub.3 receptors (for example, those existing in human cerebral cortex) than its antagonistic effect against 5HT.sub.1 receptors (for example, those existing in mouse ventral spinal marrow) and 5HT.sub.2 receptors (for example, those existing in human smooth muscle). The receptor antagonist is abbreviated as an antagonist in this invention.
Preferred examples of the 5HT.sub.3 antagonist are ester(common name, Tropisetron), endo-3,5-dichlorobenzoic acid methyl!-4H-carbazol-4-one.multidot.hydrochloride dihydrate (common name, -1H-indazole-3-carboxamide (common name, nzimidazole.multidot.hydrochloride(common name, YM-060), (+)-8, FR), etc., which, however, are not limitative, but any other known or novel 5HT.sub.3 antagonists can be used in the present invention. For example, compounds disclosed in the following patent publications are known. European Patent Laid-Open No.
REFERENCES:
patent: 4695578 (1987-09-01), Coates et al.
patent: 4914107 (1990-04-01), Cohen et al.
patent: 5141945 (1992-08-01), Kato et al.
patent: 5173493 (1992-12-01), Kato et al.
patent: 5290785 (1994-03-01), Kato et al.
patent: 5300645 (1994-04-01), Audia et al.
patent: 5607938 (1997-03-01), Katsuta et al.
U.S. application No. 08/736,248, filed Oct. 24, 1996, Pending.
U.S. application No. 08/793,798, filed Mar. 17, 1997, Pending.
Nomura Kazuhiko
Yamaguchi Isamu
Cintins Marianne M.
Fujisawa Pharmaceutical Co. Ltd.
Moezie M.
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