37 results about "5-HT2C receptor" patented technology

The subject invention provides methods for treating symptoms and/or conditions associated with idiopathic hyperhidrosis by using compounds that decrease the activity of serotonin 5-HT2C receptors. Compounds that can ameliorate symptoms of idiopathic hyperhidrosis and associated conditions include 5-HT2C receptor antagonists (i.e., ketanserin, ritanserin, mianserin, mesulergine, cyproheptadine, fluoxetine, mirtazapine, olanzapine, and ziprasidone) as well as 5-HT2C receptor modulators (i.e., inverse agonists, partial agonists, and allosteric modulators).

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

[Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

[Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT_2B receptor and 5-HT₇ receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT_2C receptor activation action and the like.

A 5-HT_2C receptor activator containing a compound represented by the formula (I):

wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

The present invention relates to the use of certain 5-HT2C receptor antagonists in the manufacture of medicaments for the treatment of mental disorders, in particular aspects of schizophrenia, cognitive impairment and suicidality, as well as to methods for determining the suitability of compounds for such a use.

Disclosed is a pharmaceutical composition for prophylaxis and treatment of pancreatitis comprising a 5-HT2A receptor antagonist as an effective component, wherein the binding activity (pKi) of the 5-HT2A receptor antagonist to a 5-HT2A receptor is higher at least by 1.0 than the binding activities to a 5-HT2B receptor and a 5-HT2C receptor. Preferably the binding activity (pKi) of the 5-HT2A receptor antagonist to the 5-HT2A receptor is at least 7.0, and more preferably at least 8.0. The present invention also provides a method of identifying a candidate substance for prophylactic and therapeutic agent for pancreatitis, comprising determining whether a test substance has a 5-HT2A receptor antagonistic activity.

Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds (I) which act at the 5HT2A receptors. This new class encompasses the candidate compounds. In Formula (A) W is F, Cl, Br, I, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; X is O or S or NR<2>; Y is NR<3>R<4>, or (CH2)mR<5>, or O(CH2)nR<6>; m is an integer between 0 and 4, inclusive; n is an integer between 0 and 4, inclusive; Z is H, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; R<1>, R<2>, R<3> and R<10> are as defined in the application.

The present invention provides a bicyclic heterocyclic compound having a serotonin 5-HT_2C receptor activation action and the like.

A compound represented by the formula (I):

wherein each symbol is as defined in the specification, or a salt thereof.

The invention belongs to the field of pharmacy, relates to medicinal use of an indole piperazine derivative, and in particular relates to appetency of the indole piperazine derivative to dopamine D3 receptor and 5-HT1A and 5-HT2A receptors, function characteristics and use in preparation of medicines for nervous system disease; adrenergic beta-2 receptor crystal structure is used as a template for the construction of a dopamine 5-HT1A receptor model; by accuracy verification on the receptor model and molecular dynamics simulation, a flexible receptor conformation can be obtained; active sites of the flexible receptor conformation can be detected; detection results are superimposed and a dynamic receptor effective-mass model is constructed; an existing compound database is screened and the activity is tested; and results show that the screened compound FDFWHF003 and its derivatives have good activity to the dopamine receptor and 5-HT receptors, can be used for preparation of anti-schizophrenia medicines, and especially is suitable for the preparation of medicines for treating schizophrenia caused by dopamine system and 5-HT system functional disorders.

The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT_2B receptor, pharmaceutical compositions comprising these compounds and their use as a medicine.

The invention provides an application of radix bupleuri total saponin and monomer saponin thereof in preparation of medicines for preventing and treating obesity, and a pharmaceutical composition taking the radix bupleuri total saponin and the monomer saponin as active components. A pharmacological experiment proves that the radix bupleuri total saponin and a monomer compound thereof have obvious agonist activity on a 5-HT2C receptor, has obvious effects of inhibiting appetite and inhibiting weight gain on SD rats in an animal experiment, and can be applied to prevention and treatment of obesity.

The invention relates to application of tricyclic chinoline and quinoxaline derivatives as well as a pharmaceutical composition containing the tricyclic chinoline and quinoxaline derivatives as a modifier, in particular agonists or partial agonists of a 5-HT2C receptor, application of the tricyclic chinoline and quinoxaline derivatives to preparing drugs for preventing or treating regulation response conditions and diseases of the 5-HT2c receptor, a method used for preventing or treating the regulation response conditions and diseases of the 5-HT2c receptor, and a method for preparing the compounds and the composition.

The invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as described in the specification, which compounds are ligands to the serotonin 5-HT2c receptor.