Delving into the Latest Updates on Pyrilamine Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Mepyramine, Mepyramine Maleate, N',N'-dimethyl-N-(p-methoxybenzyl)-N-(2-pyridyl)ethylenediamine

+ [7]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication

HypersensitivityPruritus

Inactive Indication-

Originator Organization

Impax Laboratories LLC

Active Organization

Impax Laboratories LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (07 Aug 1973),

HypersensitivityPruritus

Regulation-

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Structure

Molecular FormulaC17H23N3O

InChIKeyYECBIJXISLIIDS-UHFFFAOYSA-N

CAS Registry91-84-9

View All Structures (2)

The present project is a human experimental study. The aim is to assess the pharmacologically modulated excitability of peripheral sensory nerves with a human experimental model.
The study measures the excitability of peripheral sensory nerves before and after application of different topical drugs (lidocaine (5%), phenytoin (10%),mepyramine (2%) and placebo).

Start Date01 Apr 2024

Sponsor / Collaborator

University of Aalborg

NCT02601235 / CompletedPhase 3

Clinical Evaluation of Safety and Efficacy of Pediatric Naridrin in Comparison to Afrin on the Improval of Nasal Congestion.

The purpose of this study is to evaluate the efficacy of the Naridrin in improving nasal congestion.

Start Date16 Jan 2018

Sponsor / Collaborator

EMS SA (Brazil)

100 Clinical Results associated with Pyrilamine Maleate

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100 Translational Medicine associated with Pyrilamine Maleate

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100 Patents (Medical) associated with Pyrilamine Maleate

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3,395

Literatures (Medical) associated with Pyrilamine Maleate

01 Nov 2024·Bioorganic & Medicinal Chemistry Letters

Design, synthesis and antitumor activity of novel 4-oxobutanamide derivatives

Article

Author: Jiang, Zirui ; He, Jingliang ; Li, Hanxue ; Zhang, Siyi ; Gu, Yifei ; Chen, Jiayin ; Dong, Xue ; Wu, Caiju ; Wang, Siqi ; Ji, Jing ; Yan, Lili ; Wang, Ruiying ; Liu, Zhiyu ; Wang, Xiaoshuo ; Zhang, Luyao

To find highly effective and low-toxicity antitumor drugs to overcome the challenge of cancer, we designed and synthesized a series of novel 4-oxobutanamide derivatives using the principle of molecular hybridization and tested the antiproliferative ability of the title compounds against human cervical carcinoma cells (HeLa), human breast carcinoma cells (MDA-MB-231) and human kidney carcinoma cells (A498). Among them, N¹-(4-methoxybenzyl)-N⁴-(4-methoxyphenyl)-N¹-(3,4,5-trimethoxyphenyl) succinimide DN4 (IC₅₀ = 1.94 µM) showed the best proliferation activity on A498, superior to the positive control paclitaxel (IC₅₀ = 8.81 µM) and colchicine (IC₅₀ = 7.17 µM). Compound DN4 not only inhibited the proliferation, adhesion and invasion of A498, but also inhibited angiogenesis and tumor growth in a dose-dependent manner in the xenograft model of A498 cells. In addition, we also predicted the physicochemical properties and toxicity (ADMET) of these derivatives, and the results suggested that these derivatives may have the absorption, distribution, metabolism, excretion, and toxicity properties of drug candidates. Thus, compound DN4 may be a promising drug candidate for the treatment of cancer.

01 Oct 2024·Pharmacology Research & Perspectives

Histamine H₁‐receptor‐mediated modulation of NMDA receptors signaling responses

Article

Author: Arrang, J.‐M. ; Armand, V.

AbstractThis study attempted to clarify the role of histamine H1 receptors in epilepsy by exploring the effects of agonists and inverse agonists on the rundown of the current induced by iterative applications of NMDA or GABA in primary neuronal culture. Mepyramine, a classical H1‐receptor antagonist/inverse agonist, increased the NMDA current by about 40% during the first minutes of recording. This effect was concentration‐dependent, maximal at 10 nM, and mimicked by triprolidine, another antagonist/inverse agonist. No endogenous histamine was detected in the cultures by a selective immunoassay; both compounds were acting as inverse agonists. Indicating a high constitutive activity of the H1 receptor in this system, histamine did not affect the NMDA rundown, including its settlement, but significantly reversed the effect of mepyramine. A similar pattern was obtained with 2,3 bromophenyl histamine, a selective H1‐receptor agonist. The initial increase induced by the two inverse agonists was followed by the same rundown as in controls. H1‐ and NMDA receptors are colocalized in most cultured neuronal cells. Mepyramine and histamine did not affect the GABA rundown. Our findings suggest an interaction between H1‐ and NMDA receptors. Inactivation of the H1‐receptor by its inverse agonists delays the settlement of the NMDA rundown, which may underlie their proconvulsant effect reported in clinics. Therefore, H1‐receptor constitutive activity and the effect of histamine revealed in its absence, tend to facilitate the initiation of the rundown, which is consistent with the anticonvulsant properties of histamine via activation of H1‐receptors reported in many studies.

01 Oct 2024·European Journal of Pharmacology

The role of heterodimers formed by histamine H3 receptors and dopamine D1 receptors on the methamphetamine-induced conditioned place preference

Article

Author: Liu, Yu ; Zhou, Wenhua ; Li, Longhui ; Lin, Shujun ; Si, Zizhen ; Qian, Liyin ; Gong, Xinshuang ; Yu, Zhaoyin ; Ruan, Yuer ; Fan, Runyue

RATIONALEThe rewarding effect of Methamphetamine (METH) is commonly believed to play an important role in METH use disorder. The altered expression of dopamine D1 receptor (D1R) has been suggested to be essential to the rewarding effect of METH. Notably, D1R could interact with histamine H3 receptors (H3R) by forming a H3R-D1R heteromer (H3R-D1R).OBJECTIVESThis study was designed to specifically investigate the involvement of H3R-D1R in the rewarding effect of METH.METHODSC57BL/6 mice were treated with intraperitoneal injections of a selective H3R antagonist (Thioperamide, THIO; 20 mg/kg), an H1R antagonist (Pyrilamine, PYRI; 10 mg/kg), or microinjections of cytomegalovirus (CMV)-transmembrane domain 5 (TM5) into the nucleus accumbens (NAc). The animal model of Conditioned Place Preference (CPP) was applied to determine the impact of H3R-D1R on the rewarding effect of METH.RESULTSMETH resulted in a significant preference for the drug-associated chamber, in conjunction with increased H3R and decreased D1R expression in both NAc and the ventral tegmental area (VTA). THIO significantly attenuated the rewarding effect of METH, accompanied by decreased H3R and increased D1R expression. In contrast, pyrilamine failed to produce the similar effects. Moreover, the inhibitory effect of THIO on METH-induced CPP was reversed by SKF38393, a D1R agonist. Furthermore, SCH23390, a D1R antagonist, counteracted the ameliorative effect of SKF38393 on THIO. Co-immunoprecipitation (CO-IP) experiments further demonstrated the specific interaction between H3R and D1R in METH CPP mice. The rewarding effect of METH was also significantly blocked by the interruption of CMV-transmembrane domain 5 (TM5), but not CMV-transmembrane domain 7 (TM7) in NAc.CONCLUSIONThese results suggest that modulating the activity of H3R-D1R complex holds promise for regulating METH use disorder and serves as a potential drug target for its treatment.

100 Deals associated with Pyrilamine Maleate

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