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Dopamine D3 acceptor portion agonist and its application

A compound and general formula technology applied in the field of D3 receptor partial agonists

Inactive Publication Date: 2007-04-18
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Our use of a D3 partial agonist to treat withdrawal-induced compulsive behaviors in morphine-addicted mice is highly effective, strongly suggesting that this new class of drug may control the addiction-driven compulsive seeking in heroin addicts drug behavior

Method used

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  • Dopamine D3 acceptor portion agonist and its application
  • Dopamine D3 acceptor portion agonist and its application
  • Dopamine D3 acceptor portion agonist and its application

Examples

Experimental program
Comparison scheme
Effect test

preparation example IV

[0133] Preparation IV: 4-(4-(2-methoxyphenyl)piperazine)butyl-1-primary amine (90-3)

[0134] The preparation method is the same as preparation I, and 2,6-dimethylaniline (86) is replaced by o-methoxyaniline (86-3) to obtain 6.5 g of light yellow oil (90-3).

preparation example V

[0135] Preparation V: N-[4-(4-(2-methoxyphenyl)piperazine)butyl]-2-naphthylcarboxamide (BP897)

[0136]

[0137] The specific experimental operation was the same as in Example 1, substituting (90-3) for (90) to obtain 0.67 g of white solid (BP897), yield 80.6%, mp 120-121°C.

preparation example VI

[0138] Preparation VI: 4-(10-methoxy-1,2,4,4a,5,6-hexahydro-pyrazine[1,2-a]quinoline-3-butyl-1-primary amine (99)

[0139]

[0140] With 8.0g 2-methyl-8-hydroxyquinoline (91), 39.5gK 2 CO 3 and 100mL of acetone, mechanically stirred at room temperature. Take 5mLCH in the dark 3 I, dissolved in 20mL of acetone, dropped into the above-mentioned reaction bottle, and mechanically stirred at room temperature for 12h in the dark. Filtration, the filtrate was concentrated to one-half, poured into 500mL ice water to precipitate a white solid, filtered, and dried to obtain 7.5g of 2-methyl-8-methoxyquinoline (92), yield 86%, mp 127 -128°C.

[0141] 2-Methyl-8-methoxyquinoline (92) 8.7g, 100mL dioxane, 5.5g selenium dioxide, under the protection of nitrogen, heated to reflux for 2h, cooled, filtered, the filtrate was concentrated to dryness, the solid weighed Crystallization gave 8.5 g of 2-formaldehyde-8-methoxyquinoline (93) in the form of yellow needles, yield 91%, mp 103-10...

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Abstract

The present invention relates to a dopamine D3 receptor portion excitant or its pharmaceutically acceptable salt and its application for curing diseases of central nervous system. Said invention also provides its chemical structure general formula, and provides detailed description.

Description

technical field [0001] The invention relates to the field of chemical medicines, in particular to a D 3 Receptor partial agonists and their applications. Background technique [0002] The dopamine receptor subtype belongs to the G protein-coupled receptor family with 7 transmembrane domains. Seeman in 1988 divided the dopamine receptor subtypes into two families according to the difference in sequence and signal transduction coupling: D 1 dopamine-like receptors including D 1 and D 5 Receptor; D 2 dopamine-like receptors including D 2 ,D 3 and D 4 receptor. D. 2 The receptor is the main binding target of traditional antipsychotic drugs, but can cause extrapyramidal side effects. D. 3 Receptors are mainly concentrated in dopamine neural pathways in the limbic system of the brain, which is associated with emotional and cognitive functions. In the nerve structure of the limbic system, there are endogenous enkephalins and endorphin neural pathways, and dopamine neuro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/13C07D471/04C07D333/38C07D209/42A61K31/496A61K31/4375A61P25/30A61P25/16A61P25/18
Inventor 吉民戴德哉蔡进戴茵华维一贾楠李铭东顾莉洁
Owner SOUTHEAST UNIV
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