苯噻啶(Pizotifen) - 药物靶点：5-HT receptor_在研适应症：血管性水肿，房性早搏，慢性荨麻疹_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Pizotifen malate、Pizotyline

+ [4]

靶点

5-HT receptor

作用机制

5-HT receptor拮抗剂(5-羟色胺受体拮抗剂)

治疗领域

免疫系统疾病神经系统疾病心血管疾病+ [2]

在研适应症

血管性水肿房性早搏慢性荨麻疹+ [3]

非在研适应症-

原研机构

在研机构

非在研机构-

最高研发阶段批准上市

首次获批日期

英国 (1974-03-15),

血管性头痛

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C23H27NO5S

InChIKeyIWAWCPZVTXCFKD-UHFFFAOYSA-N

CAS号5189-11-7

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关联

4

项与苯噻啶相关的临床试验

NCT06500624 / RecruitingN/AIIT

Comparative Efficacy of Escitalopram Monotherapy and Escitalopram in Adjuvant With Pizotifen in Depressive Disorder

To compare the efficacy of escitalopram monotherapy and combination with pizotifen in patients of major depressive disorder(MDD).The levels of depressive symptoms as measured by the Patient Health Questionnaire (PHQ-9) at base level and during follow-up.

开始日期2024-06-03

申办/合作机构

Riphah International University

NCT06158230 / Active, not recruiting临床2期IIT

Comparison of Efficacy Between Combination of Amitriptyline-propranolol and Pizotifen for Migraine Prophylaxis: A Single-blind Randomized Controlled Trial

The goal of this clinical trial is to compare efficacy and observe common adverse effects of a combination of amitriptyline-propranolol and pizotifen as prophylactic treatments for migraine. The main question it aims to answer is:
• Does pizotifen more effective than the combination of amitriptyline-propranolol in migraine prophylaxis?
Participants will be asked to :
Maintain the provided headache diary accordingly
Take supplied drugs as described during clinical visits
Contact principle investigator if there is any issues regarding drug use and/or their adverse effects

开始日期2023-03-19

申办/合作机构

Bangabandhu Sheikh Mujib Medical University

ISRCTN97360154 / CompletedN/AIIT

A double-blind parallel-group randomised placebo-controlled trial of propranolol and pizotifen in preventing migraine in children

开始日期2009-06-01

申办/合作机构-

100 项与苯噻啶相关的临床结果

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100 项与苯噻啶相关的转化医学

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100 项与苯噻啶相关的专利（医药）

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397

项与苯噻啶相关的文献（医药）

2024-03-01·Chemistry & Biodiversity

Molecular Docking and GC/MS‐Based Approach for Identification of Anxiolytic Alkaloids from Griffinia (Amaryllidaceae) Species in a Zebrafish Model

Article

作者: Florêncio Martins, Natália ; Kueirislene Amâncio Ferreira, Maria ; de Cássia Alves Pereira, Rita ; Sheila de Queiroz Souza, Ana ; Marques Canuto, Kirley ; Silva Alencar de Menezes, Jane Eire ; Leite, Elder Luis Lima ; Riceli Vasconcelos Ribeiro, Paulo ; Deusdênia Loiola Pessoa, Otília ; Silva Dos Santos, Hélcio

AbstractGriffinia gardneriana Ravenna, Griffinia liboniana Morren and Griffinia nocturna Ravenna (Amarillydaceae) are bulbous plants found in tropical regions of Brazil. Our work aimed to determine the alkaloid profiles of Griffinia spp. and evaluate their anxiolytic potential through in vivo and in silico assays. The plants grown in greenhouses were dried and their ground bulbs were subjected to liquid‐liquid partitions, resulting in alkaloid fractions that were analyzed by gas chromatography coupled to mass spectrometry (GC‐MS). Anxiolytic activity was evaluated in zebrafish (Danio rerio) through intraperitoneal injection at doses of 40, 100 and 200 mg/kg in light‐dark box test. GC‐MS analyses revealed 23 alkaloids belonging to different skeleton types: lycorine, homolychorine, galanthamine, crinine, haemanthamine, montanine and narcisclasine. The chemical profiles were relatively similar, presenting 8 alkaloids common to the three species. The major component for G. gardneriana and G. liboniana was lycorine, while G. nocturna consisted mainly of anhydrolycorine. All three alkaloid fractions demonstrated anxiolytic effect. Furthermore, pre‐treatment with diazepam and pizotifen drugs was able to reverse the anxiolytic action, indicating involving the GABAergic and serotonergic receptors. Molecular docking showed that the compounds vittatine, lycorine and 11,12‐dehydro‐2‐methoxyassoanine had high affinity with both receptors, suggesting them to be responsible for the anxiolytic effect.

2024-02-11·Journal of Biomolecular Structure and Dynamics

Synthesis and anxiolytic effect of europium metallic complex containing lapachol [Eu(DBM) ₃ . LAP] in adult zebrafish through serotonergic neurotransmission: in vivo and in silico approach

Article

作者: Ferreira, Maria Kueirislene Amâncio ; de Menezes, Jorge Fernando Silva ; Sá Pires Silva, Andrei Marcelino ; dos Santos, Hélcio Silva ; Marinho, Gabrielle Silva ; Morais Bomfim De Lima, Julia ; Marinho, Emmanuel Silva ; Aparecida Faria de Almeida, Edna ; de Menezes, Jane Eire Silva Alencar ; da Silva, Antonio Wlisses ; da Silva, Ananias Freire ; Marques da Fonseca, Aluísio

Anxiety-related mental health problems are estimated at 3.6% globally, benzodiazepines (BZDs) are the class of drugs indicated for the treatment of anxiety, including lorazepam and diazepam. However, concerns have been raised about the short- and long-term risks associated with BZDs. Therefore, despite anxiolytic and antidepressant drugs, there is a need to develop more effective pharmacotherapies with fewer side effects than existing drugs. The present work reported the synthesis, anxiolytic activity, mechanism of action in Adult Zebrafish (Danio rerio) and in silico study of a europium metallic complex with Lapachol, [Eu(DBM)₃. LAP]. Each animal (n = 6/group) was treated intraperitoneally (i.p.; 20 µL) with the synthesized complex (4, 20 and 40 mg/Kg) and with the vehicle (DMSO 3%; 20 µL), being submitted to the tests of locomotor activity and 96h acute toxicity. The light/dark test was also performed, and the serotonergic mechanism (5-HT) was evaluated through the antagonists of the 5-HTR₁, 5-HTR_2A/2C and 5-HTR_3A/3B receptors. The complex was characterized using spectrometric techniques, and the anxiolytic effect of complex may be involved the neuromodulation of receptors 5-HT3A/3B, since the pre-treatment with pizotifen and cyproheptadine did not block the anxiolytic effect of [Eu(DBM)₃. LAP], unlike fluoxetine had its anxiolytic effect reversed. In addition, molecular docking showed interaction between the [Eu(DBM)₃. LAP] and 5HT_3A receptor with binding energy -7.8 kcal/mol and the ADMET study showed that complex has low toxic risk. It is expected that the beginning of this study will allow the application of the new anxiolytic drugs, given the pharmacological potential of the lapachol complex.Communicated by Ramaswamy H. Sarma.

2024-02-01·Science of The Total Environment

Pharmaceutical residues in stranded dolphins in the Bay of Biscay

Article

作者: Orive, Gorka ; Domingo-Echaburu, Saioa ; Brodin, Tomas ; Cerveny, Daniel ; Ruiz-Sancho, Leire ; Alzola-Andres, Maitane ; Lertxundi, Unax ; Lekube, Xabier

There is a growing concern about the presence of pharmaceuticals on the aquatic environment, while the marine environment has been much less investigated than in freshwater. Marine mammals are suitable sentinel species of the marine environment because they often feed at high trophic levels, have unique fat stores and long lifespan. Some small delphinids in particular serve as excellent sentinel species for contamination in the marine environment worldwide. To the best of our knowledge, no pharmaceuticals have been detected or reported in dolphins so far. In the present study, muscle, liver and blubber samples from three common dolphins (Delphinus delphis) and seven striped dolphins (Stenella coeruleoalba) stranded along the Basque Coast (northern Spain) were collected. A total of 95 pharmaceuticals based on detectability and predicted ability to bioaccumulate in fish were included in the liquid chromatography tandem mass spectrometry (LC-MS/MS) analysis. At least one pharmaceutical was found in 70 % of the individuals. Only three of the 95 monitored pharmaceuticals were detected in dolphin's tissues. Very low concentrations (<1 ng/g) of orphenadrine and pizotifen were found in liver and promethazine in blubber. Herein, the gap in the knowledge regarding the study organisms and marine environments with respect to pharmaceutical pollution, which demands further research to understand if pharmaceuticals are a threat for these apex predators, is highlighted and discussed.

100 项与苯噻啶相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08397	苯噻啶	N02CX01	DB06153

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
血管性水肿	中国	济南永宁制药股份有限公司	1995-01-01
房性早搏	中国	济南永宁制药股份有限公司	1995-01-01
慢性荨麻疹	中国	济南永宁制药股份有限公司	1995-01-01
室性早搏	中国	济南永宁制药股份有限公司	1995-01-01
偏头痛	加拿大	Paladin Labs, Inc.	1975-01-01
血管性头痛	英国	Phoenix Labs	1974-03-15