Last update 01 Nov 2024

5-HT1D receptor x eNOS x 5-HT1B receptor

Last update 01 Nov 2024

Basic Info

Related Targets

5-HT1D receptoreNOS5-HT1B receptor

Drugs associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

NXN-188

Target

5-HT1B receptor x 5-HT1D receptor x eNOS

Mechanism

5-HT1B receptor agonists [+2]

Active Org.-

Originator Org.

NeurAxon Pharma, Inc.

Active Indication-

Inactive Indication

Migraine With Aura [+1]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

NCT00959751 / CompletedPhase 2

Phase 2 Study of the Safety and Effectiveness of a Single Oral Dose of NXN-188 for the Treatment of Moderate to Severe Migraine Headache Without Aura

This is a a multi-center, randomized, double-blind, parallel group, and placebo controlled, two-arm study of a single oral dose of NXN-188 for the treatment of acute migraine headache without aura. Up to 120 migraineurs will be enrolled. Approximately 60 subjects having a headache history of migraine without aura will complete each of the two treatment arms to evaluate NXN-188 600 mg or placebo.

Start Date01 Jul 2009

Sponsor / Collaborator

NeurAxon Pharma, Inc.

NCT00920686 / CompletedPhase 2

A Phase 2 Study of the Safety and Effectiveness of a Single Oral Dose of NXN 188 for the Treatment of Moderate to Severe Migraine Headache With Aura

NXN-188 Dihydrochloride is being developed as an immediate release oral product for the treatment of acute migraine. This study is being conducted to evaluate NXN-188 in subjects with a migraine history of aura.

Start Date01 Jun 2009

Sponsor / Collaborator

NeurAxon Pharma, Inc.

NCT00877838 / Unknown statusPhase 2IIT

A Phase 2a Study of the Safety and Effectiveness of NXN-188 for the Acute Treatment of Migraine Attacks With Aura

The following study is being conducted to explore the safety and effectiveness of a new chemical entity called NXN-188 in subjects with a history of migraine with aura. In this study subjects will treat two attacks of migraine with aura during the aura phase - once with placebo and once with NXN-188.

Start Date01 May 2009

Sponsor / Collaborator

Danish Headache Center

[+1]

100 Clinical Results associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

100 Translational Medicine associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

0 Patents (Medical) associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

Literatures (Medical) associated with 5-HT1D receptor x eNOS x 5-HT1B receptor

01 Jun 2021·European Journal of PharmacologyQ3 · MEDICINE

Role of serotonin in regulation of pancreatic and mesenteric arterial function in diabetic mice

Q3 · MEDICINE

Article

Author: Wang, Zhongli ; Shuai, Jian ; Chen, Ling ; Gao, Yufang

The aim of this study was to investigate the reaction of pancreatic and mesenteric artery to 5-hydroxytryptamine (5-HT, serotonin) and the mechanism of nitric oxide in diabetes. Diabetic mice were induced by streptozotocin through intraperitoneal injection. The vascular tension of the pancreatic, mesenteric and brain basilar arteries in diabetic and control mice were measured by myograph in the applications of angiotensin II, 5-HT, 5-HT_2A receptor agonist 2,5-dimethoxy-4-iodoamphetamine hydrochloride (DOI), 5-HT_1B/1D receptor agonist sumatriptan, 5-HT_2B receptor agonist BW723C86, 5-HT_1D receptor antagonist Palonosetron and 5-HT₂ receptor antagonist Sarpogrelate. The effect of 5-HT on arteries pretreated with L-NAME and sodium nitroprusside (SNP) on arteries pretreated with norepinephrine were measured. The mRNA expressions of eNOS, 5-HT_1B, 5-HT_1D, 5-HT_2A and 5-HT_2B in pancreatic and mesenteric arteries were measured by Real-time PCR. The concentration of 5-HT in plasma and eNOS in pancreatic and mesenteric arteries were tested. Our results showed that the tension of pancreatic and mesenteric arteries in diabetic mice impaired to 5-HT, but not Ang II, and to DOI and sumatriptan, but normalized by incubation with L-NAME. Pancreatic and mesenteric arteries showed no differences to SNP after pretreated with NE between diabetic and control mice. The mRNA of eNOS and 5-HT receptors in pancreatic and mesenteric artery showed no difference between control and diabetic mice. We conclude that the effect of 5-HT on the tension of pancreatic and mesenteric arteries decrease in diabetic mice. It may due to the decreased activity of 5-HT receptors and the activation of eNOS, which causes nitric oxide to release more and makes the tension of vessels decreased.

01 Nov 2015·Journal of EthnopharmacologyQ2 · MEDICINE

Systems pharmacology to decipher the combinational anti-migraine effects of Tianshu formula

Q2 · MEDICINE

Article

Author: Li, Yan ; Wang, Yonghua ; Yang, Ling ; Xiao, Wei ; Wang, Zhenzhong ; Pan, Yanqiu ; Chen, Su-Shing ; Chen, Xuetong ; Zhang, Shuwei ; Zhang, Jingxiao ; Zhang, Lilei

Migraine is the most common neurovascular disorder that imparts a considerable burden to health care system around the world. However, currently there are still no effective and widely applicable pharmacotherapies for migraine patients. Herbal formulae, characterized as multiple herbs, constituents and targets, have been acknowledged with clinical effects in treating migraine, which attract more and more researchers' attention although their exact molecular mechanisms are still unclear. In this work, a novel systems pharmacology-based method which integrates pharmacokinetic filtering, target fishing and network analysis was developed and exemplified by a probe, i.e. Tianshu formula, a widely clinically used anti-migraine herbal formula in China which comprises of Rhizoma chuanxiong and Gastrodia elata. The results exhibit that 20 active ingredients of Tianshu formula possess favorable pharmacokinetic profiles, which have interactions with 48 migraine-related targets to provide potential synergistic therapeutic effects. Additionally, from systematic analysis, we speculate that R. chuanxiong as the monarch herb mediates the major targets like PTGS2, ESR1, NOS2, HTR1B and NOS3 to regulate the vascular and nervous systems, as well as the inflammation and pain-related pathways to benefit migraine patients. Meanwhile, as an adjuvant herb, G. elata may not only assist the monarch herb to improve the outcome of migraine patients, but also regulate multiple targets like ABAT, HTR1D, ALOX15 and KCND3 to modify migraine accompanying symptoms like vomiting, vertigo and gastrointestinal disorders.

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