58 results about "Serotonin 1A Receptor" patented technology

The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.

The present invention relates to a compound represented by the following formula, a pharmacologically acceptable salt thereof, or a use thereof as a pharmaceutical: wherein R1 and R2 are substituents adjacent to each other, and together with two carbon atoms to each of which they attach, form a 5- to 7-membered non-aromatic carbocyclic group or the like, which may be substituted by 1 to 4 substituents selected from (1) an oxo group, (2) a hydroxyl group, and the like; R3 represents a hydrogen atom or the like; and R6 represents a hydrogen atom or the like. This compound has a superior strength of binding to a 5-HT1A receptor and an antagonism to the receptor, and is useful as an agent for treating or preventing lower urinary tract symptoms, and particularly symptoms regarding urinary storage.

The present invention relates to a substituted piperazine compound and a use method and use thereof, and further relates to a pharmaceutical composition comprising the substituted piperazine compound and use thereof, wherein the substituted piperazine compound is a compound shown as formula (I) or a stereoisomer, tautomer, nitrogen oxide, solvate, metabolism product, a pharmaceutically acceptable salt or prodrug of the compound shown as the formula (I). The substituted piperazine compound and the pharmaceutical composition comprising the substituted piperazine compound can be used to inhibit 5-hydroxytryptamine reuptake and / or 5-HT1A receptor excitement. The invention also relates to a method for making the substituted piperazine compound and the pharmaceutical composition comprising the substituted piperazine compound, and relates to the use of the substituted piperazine compound and the pharmaceutical composition comprising the substituted piperazine compound in the treatment of central nervous system dysfunction.

It is intended to provide an agent for improving motor complications accompanying levodopa treatment of Parkinson's disease, delaying the onset of motor complications accompanying levodopa treatment, and inhibiting or delaying the progression of symptoms of Parkinson's disease, comprising a compound represented by the formula (I): a pharmacologically acceptable salt thereof or a hydrate thereof. The compound of the formula (I) has serotonin 1A receptor partial agonistic activity and also has a dopamine D3 receptor agonistic activity without having a dopamine D2 receptor antagonistic activity, has an effect of improving and delaying the onset of motor complications accompanying the repetitive administration of levodopa, and is effective also in accompanying psychiatric symptoms in patients with advanced-stage Parkinson's disease.

There is provided a selective serotonin reuptake inhibitor having affinity for serotonin 1A receptors which comprises a cyclic amine represented by the formula: wherein G represents a formula (2): a prodrug of said cyclic amine, or a pharmaceutically acceptable salt of said cyclic amine or prodrug, as an active ingredient.

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.

Contemplated substituted arylpiperazinyl compounds, and most preferably 18F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.

The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.