Agent for prophylaxis or treatment of substance abuse and dependence

A medicament and alcohol technology, which is applied in the direction of drug combination, medical formula, medical preparations containing active ingredients, etc., can solve the problems of reducing alcohol consumption and increasing alcohol consumption

Inactive Publication Date: 2012-09-26
MITSUBISHI TANABE PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the first synthesized ORL-1 receptor agonist Ro64-6198 failed to reduce alcohol consumption, on the contrary, it increased alcohol consumption at higher doses (Economidou et al., Peptides 27, 3299-3306, 2006)

Method used

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  • Agent for prophylaxis or treatment of substance abuse and dependence
  • Agent for prophylaxis or treatment of substance abuse and dependence
  • Agent for prophylaxis or treatment of substance abuse and dependence

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0101] Experimental Example 1: Effect on Alcohol Withdrawal Syndrome in Wistar Rats

[0102] (experimental method)

[0103] Male Wistar rats were used in this study. according to figure 1 12-15 g / kg / body weight of alcohol was orally administered to rats within 24 hours on the first day to the second day, and within 12 hours on the third to fifth day 9-10g / kg / body weight of alcohol. 2 hours and 7 hours after the last alcohol administration, rats were orally administered 0.3 mg / kg / body weight and 1 mg / kg / body weight of Compound A, respectively. Four types of alcohol withdrawal syndrome were observed, such as vocalization, ventromedial limb retraction, tail rigidity, and tail tremor, and scored according to the following 3-level rating scale: mild=0, moderate=1, severe=3.

[0104] (result)

[0105] Such as figure 2 As shown, 0.3 mg / kg / body weight and 1 mg / kg / body weight of Compound A significantly and dose-dependently reduced ventromedial limb contraction, tail rigidity an...

experiment example 2

[0106] Experimental Example 2: Effect on alcohol intake in msP rats.

[0107] (experimental method)

[0108] Genetically selected male alcohol-preferring rats called Marchigian Sardinian alcohol-preferring (msP) rats (Addiction Biol. 11, 339-355, 2006) were used in this study. Such as image 3 As shown, rats were housed in a day and night reversed environment (lights off at 8:30 and lights on at 20:30), which could be freely selected between water and 10% alcohol, and alcohol consumption was measured every day. One hour before the beginning of the dark period and 8 hours after the beginning of the dark period, Compound A was orally administered at 0.3 mg / kg / body weight and 1 mg / kg / body weight, respectively, for 9 consecutive days.

[0109] (result)

[0110] Such as Figure 4 As shown, Compound A at 0.3 mg / kg / body weight and 1 mg / kg / body weight significantly and dose-dependently reduced alcohol consumption in msP rats. The effect was also persistent and significant up to 9...

experiment example 3

[0111] Experimental Example 3: The effect of yohimbine-induced recovery on alcohol craving behavior in msP rats

[0112] (experimental method)

[0113] Genetically selected male alcohol-preferring rats called msP rats (Addiction Biol. 11, 339-355, 2006) were used in this study. Such as Figure 5 As shown, rats were trained to voluntarily administer 10% (w / v) alcohol per day for 30 minutes following a fixed ratio 1 (FR1) reinforcement schedule, where each response resulted in an infusion of 0.1 ml of fluid. After obtaining a stable baseline of voluntary administration of 10% alcohol, rats were subjected to extinction phases of 30 min each for 15 consecutive days. The extinction phase was the same as the voluntary 10% alcohol phase, however there was no more alcohol during the extinction phase. Starting on day ten of the extinction phase, rats were divided into three groups with similar baseline responses to 10% alcohol. For six consecutive days, each group of rats was orall...

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Abstract

The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient.

Description

technical field [0001] The present invention relates to an agent for preventing or treating substance abuse and substance dependence, comprising an ORL-1 receptor agonist as an active ingredient. Background technique [0002] After cloning the δ receptor, κ receptor, and μ receptor, the opioid receptor-like 1 (ORL-1) receptor, which is the fourth member of the opioid receptor family, was also cloned in 1994 ( FEB S Lett. 347, 284-288, 1994, FEBS Lett. 341, 33-38, 1994). Although the ORL-1 receptor shares approximately 60% homology with other opioid receptors, the ORL-1 receptor Significantly different from other opioid receptors (FEBS Lett. 341, 33-38, 1994). The ORL-1 receptor is expressed in peripheral organs such as the intestine, spleen, etc., and it is also widely expressed in the central nervous system, especially in the cortex, hippocampus, hypothalamus, tonsil, and spinal cord (Eur. J. Pharmacol. 340, 1-15, 1997, Pharmacol. Rev. 53, 381-415, 2001). [0003] In 19...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/454A61P25/30A61P25/32A61P25/34A61P25/36
CPCA61K31/454A61P25/30A61P25/32A61P25/34A61P25/36
Inventor 手岛浩慈罗伯托·奇科乔波毛里齐奥·马西
Owner MITSUBISHI TANABE PHARMA CORP
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