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Treating obesity with muscarinic receptor m1 antagonists

A technology for drugs and antidepressants, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., to solve problems such as failure to treat mental illness and failure of pirenzepine to produce behavioral effects.

Inactive Publication Date: 2012-11-14
THERAKOS INC
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although pirenzepine and tirenzepine are structurally similar to tricyclic antidepressants such as imipramine, they are not known to have psychotropic effects when given orally for the treatment of peptic ulcer disease
Additionally, in early studies in mice and rats, systemically administered pirenzepine failed to produce any behavioral effects (see, Rogoz, Z., Skuza, G., Sowinska, H., Pol. J. Pharmacol .Pharm., 1981, vol.31, pp. 615-26)

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

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Embodiment 1

[0154] Antidepressant effect: The antidepressant effect of compounds was evaluated using the rat tail suspension method. The method was described by Steru et al., (Stem L, et al., Psychopharmacol 85:367-70, 1985; Stem L, et al., Prog Neuro-Psychopharmacol & Biol Psychiat 11:659-71, 1987) and later by Crowley et al. A variant of the human method (Crowley JJ, et al., Pharmacol Biochem Beh 78(2):269-74, 2004) was adapted. Seven to eight week old (25-35 g) male CD-1 mice were housed for one week prior to testing. Mice (n=8-10 / dose group) were dosed intraperitoneally (ip) or orally (po) with the drug under study and returned to their cages for appropriate pretreatment intervals (45- 60 minutes). Using adhesive tape, suspend the mouse from the tensiometer by its tail. Based on the intensity of movement recorded by the tensiometer, activity in the following 6 minutes was scored by computer: 1) immobility, 2) avoidance behavior or 3) severe avoidance behavior. Total immobility is ...

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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 entireties. [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 for the treatment of psychological disorders, including the treatment of depression. 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/00A61K45/06
Inventor 布赖恩·西德乔丹·梅哈尼克
Owner THERAKOS INC
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