Delving into the Latest Updates on DS39201083 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Action-

Mechanism-

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Pain

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization-

Inactive Organization

Daiichi Sankyo Co., Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC16H18N2O

InChIKeyVEEBOZJIPHWJSR-UHFFFAOYSA-N

CAS Registry2361560-81-6

We identified (5'S)-10'-fluoro-6'-methyl-5',6'-dihydro-3'H-spiro[cyclopropane-1,4'-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7'(1'H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic acid-induced writhing test and formalin test in ddY mice without sedation. Moreover, 22b did not exhibit mu opioid receptor agonist activity.

01 Aug 2019·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity

Q4 · MEDICINE

Article

Author: Domon, Yuki ; Shimada, Kousei ; Arita, Tsuyoshi ; Kubota, Kazufumi ; Machinaga, Nobuo ; Asano, Masayoshi

We discovered a novel compound, 5-methyl-1,4,5,7-tetrahydro-2,5-ethanoazocino[4,3-b]indol-6(3H)-one sulfuric acid salt (DS39201083), which was formed by derivatization of a natural product, conolidine. DS39201083 had a unique bicyclic skeleton and was a more potent analgesic than conolidine, as revealed in the acetic acid-induced writhing test and formalin test in ddY mice. The compound showed no agonist activity at the mu opioid receptor.

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