Delving into the Latest Updates on Dimemorfan Phosphate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

二甲啡烷磷酸盐, 磷酸二甲啡烷

+ [2]

Target

σ1 receptor

Action

agonists

Mechanism

σ1 receptor agonists(Sigma opioid receptor agonists)

Therapeutic Areas

Respiratory Diseases

Active Indication

Cough

Inactive Indication

Acute BronchitisAcute upper respiratory infectionBronchitis, Chronic+ [3]

Originator Organization

OrphanPacific, Inc.

Active Organization

OrphanPacific, Inc.

Shandong Bestcomm Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (24 May 1974),

Cough

Regulation-

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Structure/Sequence

Molecular FormulaC18H28NO4P

InChIKeyODJHDWLIOUGPPA-URVXVIKDSA-N

CAS Registry36304-84-4

View All Structures (2)

主要目的： 1.评价中国健康受试者空腹单次口服10 mg、20 mg和40 mg磷酸二甲啡烷糖浆的药代动力学特征。 2.评价中国健康受试者空腹多次口服20 mg磷酸二甲啡烷糖浆的药代动力学特征。次要目的：评价中国健康受试者单次和多次口服磷酸二甲啡烷糖浆后的安全性

[Translation]

Primary objectives: 1. To evaluate the pharmacokinetic characteristics of 10 mg, 20 mg and 40 mg of bisphosphomorph syrup after single oral administration on an empty stomach in healthy Chinese subjects. 2. To evaluate the pharmacokinetic characteristics of 20 mg of bisphosphomorph syrup after multiple oral administration on an empty stomach in healthy Chinese subjects. Secondary objectives: To evaluate the safety of bisphosphomorph syrup after single and multiple oral administration in healthy Chinese subjects.

Start Date09 May 2017

Sponsor / Collaborator

Beijing Rundekang Medical Tech. Co., Ltd.

CTR20170471

/ CompletedNot Applicable

磷酸二甲啡烷糖浆人体药代动力学研究

[Translation] Study on the pharmacokinetics of dimethomorphan phosphate syrup in healthy volunteers

考察健康成人受试者单次及多次空腹口服磷酸二甲啡烷糖浆后人体内血药浓度经时变化过程，计算相应的药代动力学参数，评价在健康成人体内的药代动力学特征，考察并评价饮食对磷酸二甲啡烷糖浆药代动力学过程的影响，为II期临床试验方案制定提供试验依据，为临床给药剂量及给药方式提供依据。

[Translation]

To investigate the time-dependent changes in blood drug concentrations in healthy adult subjects after single and multiple oral administrations of dimethomorph phosphate syrup on an empty stomach, calculate the corresponding pharmacokinetic parameters, evaluate the pharmacokinetic characteristics in healthy adults, investigate and evaluate the effect of diet on the pharmacokinetic process of dimethomorph phosphate syrup, provide experimental basis for the formulation of Phase II clinical trial plans, and provide basis for clinical dosage and administration method.

Start Date14 Feb 2017

Sponsor / Collaborator

Shandong Bestcomm Pharmaceutical Co., Ltd.

CTR20160407

/ SuspendedPhase 3

磷酸二甲啡烷糖浆治疗儿童呼吸道感染所致咳嗽的随机、双盲、安慰剂平行对照、多中心临床试验

[Translation] A randomized, double-blind, placebo-controlled, multicenter clinical trial of dimethomorphan phosphate syrup for the treatment of cough caused by respiratory tract infection in children

以安慰剂为对照，评价磷酸二甲啡烷糖浆治疗儿童呼吸道感染所致咳嗽的有效性和安全性。

[Translation]

To evaluate the efficacy and safety of dimethomorphan phosphate syrup in the treatment of cough caused by respiratory tract infection in children, compared with placebo.

Start Date10 Nov 2016

Sponsor / Collaborator

Shandong Bestcomm Pharmaceutical Co., Ltd.

100 Clinical Results associated with Dimemorfan Phosphate

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100 Translational Medicine associated with Dimemorfan Phosphate

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100 Patents (Medical) associated with Dimemorfan Phosphate

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73

Literatures (Medical) associated with Dimemorfan Phosphate

31 Dec 2024·Redox Report

Sigma-1 receptor exerts protective effects on ameliorating nephrolithiasis by modulating endoplasmic reticulum-mitochondrion association and inhibiting endoplasmic reticulum stress-induced apoptosis in renal tubular epithelial cells

Article

Author: Song, Qianlin ; Xiong, Yunhe ; Ke, Hu ; song, Chao ; Dong, Caitao ; Yang, Sixing ; He, Ziqi ; Liao, Wenbiao ; Zhou, Jiawei ; Su, Xiaozhe ; Wang, Chuan

Oxalate-induced damage to renal tubular epithelial cells (RTECs) is an essential factor in the incident kidney stone, but the specific mechanism is unclear. Recent research has pinpointed interacting areas within the endoplasmic reticulum and mitochondria, called mitochondria-associated membranes (MAMs). These studies have linked endoplasmic reticulum stress (ERS) and oxidative imbalance to kidney disease development. The sigma-1 receptor (S1R), a specific protein found in MAMs, is involved in various physiological processes, but its role in oxalate-induced kidney stone formation remains unclear. In this study, we established cellular and rat models of oxalate-induced kidney stone formation to elucidate the S1R's effects against ERS and apoptosis and its mechanism in oxalate-induced RTEC injury. We found that oxalate downregulated S1R expression in RTECs and escalated oxidative stress and ERS, culminating in increased apoptosis. The S1R agonist dimemorfan up-regulated S1R expression and mitigated ERS and oxidative stress, thereby reducing apoptosis. This protective effect was mediated through S1R inhibition of the CHOP pathway. Animal experiments demonstrated that S1R's activation attenuated oxalate-induced kidney injury and alleviated kidney stone formation. This is the first study to establish the connection between S1R and kidney stones, suggesting S1R's protective role in inhibiting ERS-mediated apoptosis to ameliorate kidney stone formation.

01 Jul 2024·Acta Pharmaceutica Sinica B

Deep simulated annealing for the discovery of novel dental anesthetics with local anesthesia and anti-inflammatory properties

Article

Author: Ye, Ling ; Yu, Xianghua ; Tan, Yongzhen ; Hai, Ao ; Miao, Zhuang ; Liu, Xianggen ; Kang, Ting ; Gai, Wenrui ; Liang, Xinhua ; Hao, Yihang ; Tang, Yaling ; Hu, Shilong ; Gan, Yu ; Ke, Bowen ; Liu, Jin ; Shi, Rongjia ; Liu, Wencheng ; Zhao, Yi ; Wang, Haofan ; Fu, Yihang

Multifunctional therapeutics have emerged as a solution to the constraints imposed by drugs with singular or insufficient therapeutic effects. The primary challenge is to integrate diverse pharmacophores within a single-molecule framework. To address this, we introduced DeepSA, a novel edit-based generative framework that utilizes deep simulated annealing for the modification of articaine, a well-known local anesthetic. DeepSA integrates deep neural networks into metaheuristics, effectively constraining molecular space during compound generation. This framework employs a sophisticated objective function that accounts for scaffold preservation, anti-inflammatory properties, and covalent constraints. Through a sequence of local editing to navigate the molecular space, DeepSA successfully identified AT-17, a derivative exhibiting potent analgesic properties and significant anti-inflammatory activity in various animal models. Mechanistic insights into AT-17 revealed its dual mode of action: selective inhibition of Na_V1.7 and 1.8 channels, contributing to its prolonged local anesthetic effects, and suppression of inflammatory mediators via modulation of the NLRP3 inflammasome pathway. These findings not only highlight the efficacy of AT-17 as a multifunctional drug candidate but also highlight the potential of DeepSA in facilitating AI-enhanced drug discovery, particularly within stringent chemical constraints.

01 Feb 2023·YAKUGAKU ZASSHI

Development of a Simple and Sensitive Enzyme-linked Immunosorbent Assay for Sinomenine

Article

Author: Kataoka, Hiroto ; Saita, Tetsuya ; Ura, Kanae

Sinomenine (SIN) is a major component contained in extracts of the Chinese medicinal herb Sinomenium acutum. SIN has various pharmacological properties, including cytoprotection, immunosuppression and anti-inflammation effects. Furthermore, recent studies have reported that SIN has anti-tumor and antidepressant effects, which has created a strong need for SIN kinetic studies. This paper reports a simple and sensitive competitive enzyme-linked immunosorbent assay (ELISA) for the pharmacokinetic evaluation of SIN. Anti-SIN serum was obtained by immunizing mice with an antigen conjugated with bovine serum albumin and carboxylic modified SIN using the N-succinimidyl ester method. Enzyme labeling of SIN with horseradish peroxidase was similarly performed using carboxylic modified SIN. Under optimized conditions, this ELISA shows a linear detection range from 40 to 5000 pg/mL, and a limit of detection of 12.1 pg/mL for 50-µL samples. This assay was specific for SIN and showed very slight cross-reactivity with dextromethorphan (0.45%), dimemorfan (0.22%) and codeine (0.01%), but no cross-reactivity with 2-methoxycyclohex-2-enone (<0.001%). Using this ELISA, SIN levels were easily determined in the blood of mice after oral administration of Kampo medicine, Boiogito. The ELISA may be a valuable tool for studies of the biological and pharmacological properties of SIN.

100 Deals associated with Dimemorfan Phosphate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Dimemorfan Phosphate	R05DA11	DB13810

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cough	Japan	OrphanPacific, Inc.	24 May 1974

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Cough	Phase 3	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	19 Sep 2013
Acute Bronchitis	Phase 2	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	10 Nov 2016
Acute upper respiratory infection	Phase 2	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	10 Nov 2016
Pneumonia	Phase 2	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	31 Jul 2014
Bronchitis, Chronic	Phase 1	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	31 Jul 2014
Silicotuberculosis	Phase 1	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	31 Jul 2014
Dry cough	Phase 1	China	Shandong Bestcomm Pharmaceutical Co., Ltd.	19 Sep 2013