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72 results about "Tryptamine Receptors" patented technology

N,N-disubstituted diazocycloalkanes

N,N-Disubstituted diazocycloalkanes of the formula I(R1=halogen, R2=(C3–C8)-cycloalkyl, R3=(C1–C4)-alkoxy or (C1–C4)-haloalkoxy group, m is 1 or 2 and n is 1 or 2, have affinity for serotonergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor.
Owner:RECORDATI SA

Deuterium-Enriched Pyrimidine Compounds and Derivatives

ActiveUS20130040957A1Prevent proliferationBiocideSenses disorderDiseaseMalignant carcinoid tumors
The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof,and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT1, 5-HT1A, 5-HT2 receptors, 5-HT2A and 5-HT2B receptors, dopamine receptors and multiple kinase pathways.
Owner:DHANOA DALJIT SINGH

Dihydroquinazolinones as 5HT modulators

The present application provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
Owner:BRISTOL MYERS SQUIBB CO

Benzoyl-piperidine derivatives as dual modulators of the 5-HT2a and d3 receptors

The present invention relates to compounds of formula (I)wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
Owner:F HOFFMANN LA ROCHE & CO AG

Application of 3-methoxyl mangiferin in preparing medicine used for treating post-stroke depression

ActiveCN103191141AOrganic active ingredientsNervous disorderDepressions symptomsAnxiety
The invention relates to the field of medicine, and discloses a novel application of 3-methoxyl mangiferin in the field of pharmacy, and a medicine composition comprising 3-methoxyl mangiferin. 3-methoxyl mangiferin can promote hippocampus dentate gyrus neuron 5-hydroxytryptamine 1A receptor gene and protein expressions, and can induce neurotrophic effects such as hippocampus remodeling performed by 5-hydroxytryptamine. Therefore, post-stroke hippocampus nerve aregeneratory can be substantially ameliorated, 5-HT re-uptake of nerve presynaptic membrane can be selectively inhibited, 5-HT positive cell expression at hypothalamus can be reduced, exhaustion of 5-HT can be relieved, and anxiety and depression symptoms caused by 5-HT exhaustion can be relieved. Therefore, 3-methoxyl mangiferin can be used in preparing medicines used for treating post-stroke depression.
Owner:KPC PHARM INC

Medicinal composition for treating emesis

The invention provides a medicinal composition containing a neurokinin 1(NK-1) receptor antagonist, a 5-hydroxytryptamine 3 (5HT-3) receptor antagonist and adrenocortical hormone. The medicinal composition adopts a NK-1 receptor antagonist, a 5HT-3 receptor antagonist and adrenocortical hormone as active components, is added with certain auxiliaries with specific spices and proportion to prepare and develop an oral preparation according to a technical means specified in the invention. The medicinal composition can be used for preventing and treating nausea and emesis caused by cancer radiotherapy, chemotherapy and operation. The invention aims to provide a medicinal composition preparation which can prevent and treat emesis more conveniently by utilizing the NK-1 receptor antagonist, the 5HT-3 receptor antagonist and adrenocortical hormone, thereby improving the compliance of a patient.
Owner:HAISCO PHARMA GRP INC

Piperazine derivatives and applications thereof

InactiveCN101381342AInhibition of feedingGrowth inhibitionBiocideOrganic chemistryPyridinylpiperazineMechanism of action
The invention relates to a piperazine derivate and application thereof. The piperazine derivate takes N1-arylmethyl and N4-pyridyl piperazine as parent matrixes to modify the structure of pesticides of main pharmacophore of the N1-arylmethyl and N4-pyridyl piperazine, so as to obtain a type of novel compound. As shown by biological (insect disinfestation) activity determination: the novel compound designed and synthesized by the invention can effectively inhibit feeding and growth of crolepidopteron, and cause the crolepidopteron to die. The piperazine derivate not only is helpful to the further research of 5-hydroxytryptamine receptors of insects but also provides direction for creation of green pesticides with a novel functional mechanism.
Owner:EAST CHINA UNIV OF SCI & TECH

Methods and compositions for treating cancer using serotonin receptor inhibitors

The present invention provides methods for treating cancer using serotonin receptor inhibitors, such as serotonin receptor inhibitory antibodies, among others. The invention also features compositions containing serotonin receptor inhibitors, methods of diagnosing patients with serotonin receptor-associated cancer, and methods of predicting the response of cancer in a subject to treatment with serotonin receptor inhibitors.
Owner:FLAGSHIP PIONEERING INNOVATIONS V INC

Conformation-constrained entirely-synthetic macrocyclic compounds

The invention relates to conformation-constrained entirely-synthetic macrocyclic compounds. A conformation-constrained, space-defined 12-30-member macrocyclic system (I) which is as shown in the description comprises three different constitution units: an aromatic template a, a confor1ation regulator b and a spaced part c, which are illustrated in the description and the claims. The macrocyclic compounds (I) can be easily prepared according to a parallel synthesis method or a combinatorial chemistry method, and are designed for realizing interaction with a specific biological target. Particularly, the compounds show agonistic or antagonistic activity to the following matters: a motilin receptor (MR), a 5-hydroxytryptamine receptor (5-HT2B receptor) of a subtype 5-HT2B, and a prostaglandin F2alpha receptor (FP receptor). Thus, the compounds are effectively used for treating gastrointestinal tract hypomotility disorder such as diabetic gastroparesis and constipation-predominant irritable bowel syndrome, CNS-related diseases such as migraine, schizophrenia, psychosis and depression, ocular hypertension such as glaucoma-related ocular hypertension, and premature delivery.
Owner:POLYPHOR AG

Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors

The present invention relates to compounds of formula (I)wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
Owner:F HOFFMANN LA ROCHE & CO AG

5-halo-tryptamine derivatives used as ligands of 5-HT 6 and/or 5-HT7 serotonin receptors

Compounds of Formula (I): (I); wherein: R1 and R2 either the same or different, are H or linear or branched C1-C6 alkyl; R3=linear or branched C1-C6 alkyl; R4=halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HT6 and / or 5-HT7 serotoninergic receptors.
Owner:SIGMA TAU IND FARMACEUTICHE RIUNITE SPA

Indazole- and pyrrolopyridine-derivative and pharmaceutical use thereof

InactiveUS20140057895A1Excellent brain penetrationBiocideNervous disorderTryptamine ReceptorsPharmaceutical Substances
The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.
Owner:SUMITOMO DAINIPPON PHARMA CO LTD

1-[(4-hydroxypiperidine-4-yl) methyl] pyridine-2(1H)-one derivatives, preparation method and use thereof

The present invention relates to N-[(4-hydroxypiperidine-4- Base) methyl] pyridin-2 (1H)-one derivatives, their stereoisomers, their pharmaceutically acceptable salts and their solvates, and their preparation methods, and their use in the prevention or treatment of 5-HT system dysfunction Related central nervous system diseases such as depression, anxiety, cognitive deficits, mania, schizophrenia, pain, etc., or used as a tool drug to study 5-HT function and its 5-HT dysfunction related diseases, and pharmaceutical compositions containing these compounds. Each substituent in formula I is as described in the specification.
Owner:INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A

Sulfonyl fluoride compound and application thereof

The invention discloses a sulfonyl fluoride compound. Compared with reported PET imaging agents for targeted amino acid transporter, fibroblast activating protein, vesicular monoamine transporter 2, serotonin receptor and prostate specific membrane antigen protein change related diseases, the series of sulfonyl fluoride compounds designed and synthesized by the invention have the advantages of simple labeling conditions, high yield and high affinity. The invention belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine.
Owner:首都医科大学脑重大疾病研究中心

Tc-labeled arylpiperazine derivatives for imaging serotonin receptor

The present invention relates to Tc-labeled arylpiperazine derivatives for imaging serotonin receptor and, more particularly, to arylpiperazine derivatives coupled with MAMA-disulfide, N2S2 or dimethyl-N2S2 chelating ligand represented by the following chemical formula (1). New arylpiperazine derivatives according to the present invention have no problem of amide hydrolysis in metabolism and have a high affinity for serotonin receptors, and can be labeled with an optimum radionuclide of technetium, thereby being usefully applied for monitoring neurodegenerative diseases or neurological diseases of a mammal.
Owner:KOREA ATOMIC ENERGY RES INST

Compound having dual functions to 5-HT and application thereof in depressive disorder treatment

The invention discloses a compound having dual functions to 5-HT and application thereof in depressive disorder treatment. The formula is shown in the description, wherein R1, R2, R3 and R4 are independently selected from H, F or OH. In recent years, an antidepressant having the dual functions of 5-hydroxytryptamine 1A acceptor partial agitation and selective 5-hydroxytryptamine re-uptake inhibition becomes a hot point direction of a novel antidepressant drug research. In a [3H]5-HT uptake inhibiting effect experiment of a rat synaptosome and a h5-HT1A combined affinity experiment, the compound is verified to have the 5-HT re-uptake inhibiting effect and the agitating effect to a 5-HT1A acceptor. The fact that the compound can be used as a drug for treating human central nervous system disorders, such as a depressive disorder and an anxiety disorder, is demonstrated.
Owner:郝惠敏

New function of Dittany Bark active component for promoting increment expression of 5-hydroxytryptamine

Dittany Bark is an important traditional Chinese medicinal material. The invention discloses a new function of a Dittany Bark active component. The experiment on the action of the Dittany Bark active component on rat primary culture neurons detects that the Dittany Bark active component can promote overexpression of 5-hydroxytryptamine receptor gene 5HTR1A. Since the 5-hydroxytryptamine can have important influence on emotions, memory and other behaviors of neurons, the result indicates that the Dittany Bark active component can promote the changes of human hedonia, long-time-interval memory and other functions.
Owner:泰州市新滨江开发有限责任公司

Use of 5-hydroxytryptamine receptor subtypes 3 and 4 and antagonists thereof in treatment of post-cholecystectomy diarrhea

The invention discloses an application of 5-hydroxytryptamine receptor subtypes 3 and 4 as drug targets in treatment of post-cholecystectomy diarrhea, and an application of an antagonist of the 5-hydroxytryptamine receptor subtypes 3 and 4 in treatment of post-cholecystectomy diarrhea. According to the application disclosed by the invention, intestinal flora change after cholecystectomy is one of pathogenic factors causing postoperative diarrhea, and diarrhea is mainly caused by accelerated peristalsis of colon, so that synthesis increase of 5-HT is an important factor for accelerated peristalsis of colon, the expression quantities of receptors 5-HT3 and 5-HT4 subtypes of 5-HT are obviously increased, and the 5-HT can be used as a potential treatment target. A diarrhea model mouse is treated by adopting two 5-HT receptor inhibitors, namely psilosetron and GR113808, and a relatively good curative effect is achieved.
Owner:上海市闵行区中心医院

Flunarizine derivative, preparation method and use thereof

InactiveCN103130746AOrganic chemistryMetabolism disorderSide effectExtrapyramidal system
The invention discloses flunarizine derivative, a preparation method and use of the flunarizine derivative. The flunarizine derivative, the preparation method and the use of the flunarizine derivative are specially characterized in that halogen is used to replace hydrogen, tri-flunarizine and chlorine flunarizine on specific loca, wherein the tri-flunarizine is (E)-1-[double(4- fluorinated phenyl)methyl]4-[2-allyl-3-(4-fluorinated phenyl)]-piperazine, and the chlorine flunarizine is (E)-1-[double(4-fluorinated phenyl)methyl]4-[2-allyl-3-(4-chlorphenyl)]-piperazine. Hydroxylation metabolism of carbon atoms on corresponding loca is blocked. Compared with the flunarizine, the derivative has stronger antagonism of calcium ion and weak antagonism of 5-hydroxytryptamine receptor, and extrapyramidal system reaction and other side effects in a clinical using process are avoided under the premise of improving pharmaceutical activity.
Owner:王化录

Lorcaserin hydrochloride jelly and preparation method thereof

A lorcaserin hydrochloride jelly and a preparation method thereof are disclosed. Jelly is a leisure food, which is welcome by the young, but the young is prone to obesity. Jelly is delicious, normally the intake amount is large, but jelly contains very few calories. The jelly is a food for reducing fat when jelly does not affect the normal functions of digestion system. Lorcaserin chloride is a 5-hydroxy tryptamine (5-HT) acceptor stimulant, and can be used as an auxiliary drug for treating chronic weight gain by reducing the diet calories and increasing the body movement. Lorcarserin hydrochloride is made into jelly so that a user can enjoy the delicious taste of jelly and is capable of reducing the weight at the same time, and the treatment and delicious taste are perfectly combined.
Owner:BEIJING SUNHO PHARMA

Pyrrolothiazine and pyrrolothiazephine compounds having serotonin-2 receptor antagonistic and alpha-1-blocking action

InactiveUS20050038242A2Strong serotonin- receptor antagonistic actionLow toxicityBiocideOrganic chemistrySide effectHeart disease
Abstract of the Disclosure A pyrrolesulfonamide derivative, Compound (I), which has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
Owner:ASUBIO PHARMA

The serotonin receptor gene pr5-ht8 of Pieris rapae and its application

The invention relates to the fields of the molecular biology, the cell biology and the agricultural pharmacology, mainly relates to a novel 5-hydroxytryptamine acceptor gene expressed in cabbage caterpillar, and its coding protein, and also relates to a use of the protein and the acceptor gene in the detection of the screening and / or the evaluation of substances for regulating the activity of a 5-hydroxytryptamine acceptor. The above detection method sequentially comprises the following steps: 1, transferring a recombinant vector containing the cabbage caterpillar 5-hydroxytryptamine acceptor gene Pr5-HT8 to a host cell line; 2, processing cells obtained in step 1 by a candidate substance; and 3, detecting the change of the concentration of calcium ions in cells obtained in step 2, wherein the rise of the concentration of the calcium ions in the cells shows that the candidate substance can activate the expressed target acceptor Pr5-HT8.
Owner:ZHEJIANG UNIV

Novel application of high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909

The invention relates to a novel application of a high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909. A molecular formula of the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 is C14H18N2, the molecular weight is 214.30600, and the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 is white powder and has good water solubility. The invention discloses the application of the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 in preparation of medicines for inhibiting addiction and withdrawl reactions of opioid substances such as morphine, or the application in preparation of the medicines for inhibiting the addiction and withdrawl reactions of morphine substances. According to the novel application disclosed by the invention, the latest researches show that WAY163909 (0.5-1.0mg / kg) can be used for significantly reducing the horizontal movement distance, horizontal movement speed and the withdrawal reactions of mice after morphine-dependent mice are subjected to naloxone precipitation. The novel application disclosed by the invention discovers that WAY163909 can be used for rescuing and treating the addiction and withdrawl reactions produced by the opioid substances such as morphine in clinical treatment and can be used for treating the possible recurrences for the first time.
Owner:ANHUI MEDICAL UNIV

Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof

The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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