Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1995-07-24
1997-04-01
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A01N 3712, A61K 31195
Patent
active
056166184
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/00120.
TECHNICAL FIELD
The present invention relates to a medical use of threo-3-(3,4-dihydroxyphenyl)serine (hereinafter abbreviated as threo-DOPS). More particularly, the present invention relates to a medical use of threo-DOPS as an analgesic drug, especially in the treatment of acute and chronic pains or continuous pains.
BACKGROUND ART
Analgesic drugs are roughly classified into a narcotic type and a non-narcotic type. The latter type of analgesics have been widely employed for clinical use due to their safety and easy manipulation.
In terms of clinical classification, there are two types of pains, i.e., acute pains and chronic or continuous pains. Acute pains are induced by specific causes such as wound and inflammation. Conventional analgesics have all been developed and clinically used for acute pains. On the other hand, chronic pains involve continuous pains over more than 6 months to a few years even after wounds causing acute pains have been healed. For such chronic pains, conventional analgesics are not always effective. A variety of drugs such as antidepressants and antispasmodics are applied to relieve chronic pains but there has been no decisive drug so far [Hiroshi Takagi, "Kyuseitsu-oyobi-Manseitsuno-Yakuri (Pharmacology of acute and chronic pains)", Nihon Ishikai Zasshi, Vol. 104, No. 1, pages 37-41, 1990].
Therefore, an object of the present invention is to provide an analgesic drug which is different from known analgesics in the action mechanism and is effective not only for acute pains but also for chronic pains.
DISCLOSURE OF INVENTION
The present inventors have made extensive studies to achieve the foregoing object. As a result, it has been discovered that a pharmaceutical composition comprising threo-DOPS as an effective ingredient exhibits an analgesic activity to relieve chronic or continuous pain as well as acute pain. The present invention has thus been accomplished.
That is, the present invention relates to an analgesic composition comprising as an effective ingredient threo-DOPS or a pharmaceutically acceptable acid addition salt thereof.
The present invention also relates to a method for the treatment of diseases with pains which comprises administering to human an effective dose of threo-DOPS or a pharmaceutically acceptable acid addition salt thereof.
The present invention further relates to use of threo-DOPS or a pharmaceutically acceptable acid addition salt thereof in the production of an analgesic composition.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 shows the results of the analgesic effect of L-threo-DOPS assessed by the tail flick method.
FIG. 2 shows the results of the analgesic effect of L-threo-DOPS assessed by the kaolin-induced writhing test.
FIG. 3 shows the results of the analgesic effect of L-threo-DOPS assessed by the formalin-induced encroachment test.
FIG. 4 shows the results of morphine antagonist, naloxone, on the analgesic effect of L-threo-DOPS assessed by the tail flick method and the kaolin-induced writhing test.
FIG. 5 shows the results of adrenaline blocking agent, phentolamine, on the analgesic effect of L-threo-DOPS assessed by the tail flick method.
FIG. 6 shows the results of decarboxylase inhibitor, benserazide, on the analgesic effect of L-threo-DOPS assessed by the tail flick method.
FIG. 7 shows the results of the analgesic effect of L-threo-DOPS by oral administration, which was assessed by the tail flick method.
BEST MODE FOR CARRYING OUT THE INVENTION
Threo-DOPS used in the present invention is a known compound represented by the following formula: ##STR1## This compound may be prepared according to known methods as reported in Japanese Patent Application KOKOKU No. 1-49139 and U.S. Pat. No. 4,480,109. Threo-DOPS has optically active L- and D-forms and racemic DL-form. Among them, L-threo-DOPS is preferred for the purpose of the present invention. Since 1989, L-Threo-DOPS has been clinically applied to improve freezing gait observed in Parkinson's disease.
In the present invention, threo-D
REFERENCES:
patent: 4529603 (1985-07-01), Mori et al.
patent: 4647587 (1987-03-01), Katsube et al.
Cook Rebecca
Sumitomo Pharmaceuticals Company Limited
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