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Benzylisoquinoline derivative- or bisbenzylisoquinoline derivative-containing psychotropic agent, analgesic and/or antiphlogistic, and health food

a technology of bisbenzylisoquinoline and psychotropic agent, which is applied in the field of bisbenzylisoquinoline derivative or bisbenzylisoquinoline derivativecontaining psychotropic agent, analgesic and/or antiphlogistic, and health food, can solve the problems of complex symptoms, serious social problems, and sickness that is yet to be clearly understood, so as to achieve small adverse reactions, reduce pain and inflammation, and reduce the effect of side effects

Inactive Publication Date: 2007-02-01
EDUCATION CENT OF TRADITIONAL CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a psychotropic agent, a health food with psychotropic action, and an agent with analgesic and antiinflammatory actions, all containing a benzylisoquinoline or bisbenzylisoquinoline derivative derived from lien tzehsin. These compounds are safe and effective even when taken for an extended period of time. The invention also provides methods for preventing or treating various psychiatric disorders, pain, and inflammation using these compounds. The invention provides a natural and safe alternative to existing drugs used for these purposes."

Problems solved by technology

The psychiatric disorders raise a serious social problem as the patients are inadaptable with society, and also an important issue from the viewpoint of medical economy.
These symptoms often appear in a complicated way.
However, the causes of the sickness are yet to be clearly understood, and the claim that schizophrenia is a single disease is still under a cloud.
Drugs that have an action on the intracerebral dopamine nervous system have been used for treatment of schizophrenia, but also raised problems of extrapyramidal tract disorders (parkinsonian syndromes) as the adverse reactions, i.e., the adverse reactions observed as catalepsy in animal experiment systems.
However, these drugs also carry the problem of side reactions such as motor coordination disorder, induction of catalepsy, and convulsive action induced by strychnine or picrotoxin.
However, it is pointed out that tricyclic or similar cyclic antidepressants cause anticholinergic actions such as dry mouth, eye adjustment disorder (misty vision), constipation, and dysuria, increase in body weight presumably caused by the antihistamic action, adrenolytic actions such as hypotension, dizziness, and stagger, adverse reactions such as cardiotoxic diseases, as well as acute poisoning by excessive intake.
However, a component contained in Saint John's Wort is known to have a serious adverse reaction, photohypersensitivity, and another component a side reaction affecting the kinetics of cyclosporine metabolism in the body.
Narcotic analgesic agents including morphine exhibit a strong analgesic action through opioid receptor in central nervous system but have a problem that they are likely to cause a drug dependence.
However, non-steroidal antiinflammatory agents are prone to frequently cause side effects such as stomach disorders with increasing efficacy.
However, there are no known reports about the pharmacological effects of lien tzehsin components other than those described above.

Method used

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  • Benzylisoquinoline derivative- or bisbenzylisoquinoline derivative-containing psychotropic agent, analgesic and/or antiphlogistic, and health food
  • Benzylisoquinoline derivative- or bisbenzylisoquinoline derivative-containing psychotropic agent, analgesic and/or antiphlogistic, and health food
  • Benzylisoquinoline derivative- or bisbenzylisoquinoline derivative-containing psychotropic agent, analgesic and/or antiphlogistic, and health food

Examples

Experimental program
Comparison scheme
Effect test

example 1

(Evaluation of Sedative Action)

[0142] Twenty five mice were grouped into five groups each having five mice, to which 5 mg / kg of N-methylcoclaurine hydrochloride (treatment group 1-1: i.p. administration), 50 mg / kg of neferine hydrochloride (treatment group 1-2: oral administration, and treatment group 1-3: i.p. administration), 50 mg / kg of liensinine hydrochloride (treatment group 1-4: oral administration), or physiological saline (negative control group 1-1: i.p. administration) was administered. The ultromotivity of the mice was analyzed by using a locomotor activity monitoring system (NS-AS01, Neuroscience Inc.). The ultromotivity measurements were performed at an interval of 5 minutes for 60 minutes, and the ultromotivity was judged from the count at each measuring time. The results are summarized in TABLE 1.

TABLE 1Ultromotivity (count)30Test groupminutes60 minutesTreatment group 1-1 (N-methylcoclaurine, i.p.)250250Treatment group 1-2 (neferine, oral)500750Treatment group 1-...

example 2

(Evaluation of Sleep-Enhancing Action)

[0146] Actions on thiopental sleep by various compounds were evaluated. Thiopental dissolved in physiological saline was administered intraperitoneally into mice at a dose of 60 mg / kg. 50 mg / kg of neferine hydrochloride (treatment group 2-1, n=9), 50 mg / kg of isoliensinine hydrochloride (treatment group 2-2, n=9), 100 mg / kg of lien tzehsin 2 extract hydrochloride (treatment group 2-3, n=9), only physiological saline (negative control group, n=6), or 1 mg / kg of diazepam (positive control group, n=9) was administered intraperitoneally into the mice 15 minutes before the thiopental administration. The time when the righting reflex of the mice disappeared after thiopental administration was designated as sleep-induction time and the time when the righting reflex was restored was designated as awakening time, and total sleep time was calculated from these values. The results are summarized in TABLE 3.

TABLE 3Total sleep timeTest group(min)Treatmen...

example 3

[0148] (Evaluation of the Effects on Mental Excitement of the Patients with Schizophrenia)

[0149] The effects of neferine on suppression of the enhancement of ultromotivity by methamphetamine were evaluated.

[0150] Fifteen mice were grouped into three groups of five mice, to which 50 mg / kg of neferine hydrochloride (treatment group 3-1), 100 mg / kg of the same (treatment group 3-2), and only physiological saline (negative control group) were administered respectively intraperitoneally. Methamphetamine (1 mg / kg) was administered 15 minutes after the administration. After administration of methamphetamine, each of the mice was placed in a transparent polycarbonate cage (22.5 cm×33.8 cm×14.0 cm), where the ultromotivity of the mouse was analyzed for 60 minutes by using a locomotor activity analyzer (NS-AS01, Neuroscience Inc.).

[0151] The results are summarized as ultromotivity count in TABLE 4.

TABLE 4UltromotivityTest group(count)Treatment group 3-1 (neferine 50 mg)2600Treatment grou...

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Abstract

A psychotropic agent, analgesic and / antiinflammatory agent, or health food which is safe even when taken for an extended period of term, comprising as an effective ingredient a benzylisoquinoline derivative represented by general formula (I): or a bisbenzylisoquinoline derivative represented by general formula (II): or a pharmaceutically acceptable salt thereof.

Description

TECHNICAL FIELD [0001] The present invention relates to a psychotropic agent, an analgesic agent and / or an antiinflammatory agent, or a health food which agent or food contains a benzylisoquinoline or bisbenzylisoquinoline derivative derived from lien tzehsin; use of the derivative for the manufacture of a psychotropic agent, an analgesic agent and / or an antiinflammatory agent, or a health food; and a method for preventing or treating a psychiatric disorder, a pain and / or an inflammation. BACKGROUND ART [0002] Psychiatric disorders are steadily increasing, reflecting the recent stressful society. The psychiatric disorders raise a serious social problem as the patients are inadaptable with society, and also an important issue from the viewpoint of medical economy. Drugs that are capable of affecting mental activity and behavior as the principal pharmacological action are called psychotropic drug, which are classified into schizophrenia drugs, mood-stabilizing drugs, antidepressants, ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/47
CPCA61K31/47A61K31/4709C07D217/20A61K31/4725A61K31/472A61P25/04A61P25/08A61P25/18A61P25/20A61P25/22A61P25/24A61P29/00
Inventor NAKAJIMATANAHASHI, TAKAOYAMADA, JUNSUN, SHU-JIANSUGIMOTO, YUMI
Owner EDUCATION CENT OF TRADITIONAL CHINESE MEDICINE
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