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Treating obesity with muscarinic receptor m1 antagonists

An antagonist, obesity technology, applied in the direction of application, biocide, animal repellent, etc., can solve the problems that are not disclosed or implied, the ability to hinder the sensitivity of lipogenesis

Inactive Publication Date: 2009-07-01
THERAKOS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bevan links the timing of pirenzepine administration to the timing of meals, but does not disclose or imply pirenzepine's ability to impede lipogenic sensitivity or its use to promote weight loss

Method used

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  • Treating obesity with muscarinic receptor m1 antagonists
  • Treating obesity with muscarinic receptor m1 antagonists
  • Treating obesity with muscarinic receptor m1 antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0179] Appetite Suppressant: Three month old (300-350 g) male Sprague-Dawley rats (housed individually) were used to evaluate the appetite suppressant effect of the compounds. Rats were acclimated to a "high fat" diet (BioServ Diet #F3282 or Research Diets #12451) for two weeks prior to testing (free access to food and water). The day before the experiment (at 5:00 PM), food was removed from the cage to stimulate feeding when it was returned the next morning (water supply was maintained throughout the experiment). Rats (n=8-10 / dose group) were dosed intraperitoneally (ip) or orally (po) the compound under investigation before food was provided, returned to their cages and immediately given pre-weighed food. Four hours after dosing, food was removed from cages, weighed, recorded (4 hour consumption) and returned to cages until the next morning. Twenty-four hours after dosing, the food remaining was weighed again and recorded (24-hour consumption). Cumulative consumption (expr...

Embodiment 2

[0192] Reduction of Body Weight Gain: Appetite Suppression: Three to four month old (475-550 grams) male Sprague-Dawley rats (housed individually) were used to evaluate the ability of compounds to prevent body weight gain. At the beginning of the chronic experiment, rats had been maintained (free access) on a "high fat" diet (BioServ Diet #F3282 or Research Diets #12451 ) for approximately one month. Individual body weight and water intake were recorded three times per week throughout the duration of the experiment. Two weeks after data collection, rats were weight balanced to produce test groups with equal mean body weights. Under isoflurane-induced anesthesia, rats were surgically implanted (subscapularis, subcutaneous [sc] placement) with mini-osmotic pumps (Alzet2ML2) containing appropriate drug concentrations (based on average body weight and calculated delivery duration). Alternatively, for studies using the oral route of administration, rats were dosed by daily gavage ...

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Abstract

Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application 60 / 805,066, filed June 16, 2006, and US Provisional Application 60 / 829,225, filed October 12, 2006, both of which are incorporated herein by reference in their entirety. [0003] Statement Concerning Federally Sponsored Research and Development's Rights to Inventions [0004] Not applicable field of invention [0005] The present invention relates to selective M 1 Muscarinic receptors (M 1 R) Antagonists treat obesity and promote weight loss. Background of the invention [0006] The neurotransmitter acetylcholine (ACh) interacts with two receptors in effector cell membranes: the nicotine-type receptor (nAChR), which is a ligand-gated ion channel; and the muscarinic receptor (mAChR), which It is a G protein-coupled receptor. In mammals, five mAChR subtypes have been identified, named M 1 to M 5 . m 1 Muscarinic receptors (M 1 R) is found in both th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/30A61K31/36
Inventor 布赖恩·西德乔丹·梅哈尼克
Owner THERAKOS INC
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