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Alpha 7 nicotinic agonists and antipsychotics

A technology of antipsychotics and agonists, which is especially used in the application of mental disorders, mental disorders, and the treatment of psychiatric disorders, and can solve problems such as limiting the therapeutic index of nicotinic ligands.

Inactive Publication Date: 2011-02-16
TARGACEPT INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, it would be highly desirable to provide pharmaceutical compositions and methods that incorporate a drug that interacts with nicotinic receptors but does not interact with serotonin (5HT) receptors. 3 ) receptor-interacting compounds, as cross-reactivity between these two receptor types has limited the therapeutic index of some other nicotinic ligands

Method used

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  • Alpha 7 nicotinic agonists and antipsychotics
  • Alpha 7 nicotinic agonists and antipsychotics
  • Alpha 7 nicotinic agonists and antipsychotics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0449] By combining (2S,3R)-N-(2-((3-pyridyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzo furan-2-carboxamide and clozapine to prepare a pharmaceutical composition. The compositions contain respective amounts of (2S, 3R)-N-(2-((3-pyridyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2 - formamide and clozapine, delivering a therapeutically effective amount of each component on a daily basis. The composition is administered to a patient on a once-a-day, twice-a-day, three-times-a-day, or four-times-a-day basis for the treatment of schizophrenia.

[0450] Clozapine (3.0 mg / kg) and Compound A (0.1 mg / kg) had little effect on PPI or panic when administered alone. see Figure 4 , 2a, and 2b. In contrast, there was a significant main effect (p=0.006) for the combination of clozapine (3.0 mg / kg) and Compound A (0.1 mg / kg) for the transgenic mice.

[0451] No synergy was observed in control wild-type mice. see Figure 5 and 6 .

Embodiment 2

[0453] By combining (2S,3R)-N-(2-((3-pyridyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzo furan-2-carboxamide and quetiapine to prepare a pharmaceutical composition. The compositions contain respective amounts of (2S, 3R)-N-(2-((3-pyridyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2 - formamide and quetiapine, delivering a therapeutically effective amount of each component on a daily basis. The composition is administered to a patient on a once-a-day, twice-a-day, three-times-a-day, or four-times-a-day basis for the treatment of schizophrenia.

[0454] In transgenic th(tk-) / th(tk-) mice, 3.0 mg / kg of quetiapine ( Figure 7a and 7b ) or 0.1mg / kg of Compound A ( Figure 2a and 2b ) independently has no significant main effect. However, when used in combination, there was a synergistic therapeutic effect (p=0.047) (Figure 8). [alpha]7 nicotinic agonists and antipsychotics work synergistically to increase prepulse inhibition in transgenic mice, th(tk-) / th(tk-) mice. In co...

Embodiment 3

[0460] binding assay

[0461] [ 3 H]-Methyl Nitanine ([ 3 H]-MLA) binding. [ 3 H]-Nicotine binds α4β2. NNRs were determined in rat cortical membrane preparations or SH-EP1 cells using standard methods modified from published methods (Lippiello and Fernandes, 1986). IC was determined by least squares nonlinear regression using GraphPad Prism software (GraphPAD, San Diego, CA). 50 (Concentration of compound producing 50% inhibition of binding). Using the Cheng-Prusoff equation (Cheng and Prusoff, 1973), calculate K i .

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Abstract

The present invention relates to a synergistic combination of an alpha7 (a7) nicotinic agonist and an antipsychotic agent.

Description

field of invention [0001] The present invention relates to combinations of alpha7 nicotinic agonists and antipsychotics. The invention further relates to pharmaceutical compositions comprising such combinations, and methods of treating psychiatric disorders, especially psychotic disorders, by administering said combinations. The invention further relates to kits comprising this combination, and the use of said kits in the treatment of psychiatric conditions, especially mental disorders. Background of the invention [0002] Several subtypes of neuronal nicotinic receptors (NNRs) unique to the central nervous system (CNS) have been demonstrated, the most common of which are the α4β2 and α7 subtypes. See, eg, Schmitt, Current Med. Chem. 7:749 (2000). Ligands that interact with the α7 NNR subtype have been suggested to be useful in the treatment of a variety of conditions and disorders (see Mazurov et al., Curr. Med. Chem. 13:1567-1584 (2006) and references therein). Prominen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06
CPCA61K45/06A61P25/00A61P25/18A61P25/28
Inventor M·本切里夫G·J·加托T·豪瑟K·G·乔丹S·R·莱特克沃斯
Owner TARGACEPT INC
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