Delving into the Latest Updates on Compound 49(Seoul National University) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

TRPV1 x μ opioid receptor

Action

antagonists, agonists

Mechanism

TRPV1 antagonists(Transient receptor potential cation channel subfamily V member 1 antagonists), μ opioid receptor agonists(Mu opioid receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Pain

Originator Organization

Hyper Corp., Inc.

Active Organization-

Inactive Organization

Hyper Corp., Inc.

Seoul National University

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single targeting. Based on a combination approach, a series of 4-benzyl-4-(dimethylamino)piperidinyl analogues were designed, synthesized and evaluated for their receptor activities. Among them, compound 49 exhibited the most promising dual-acting activity toward TRPV1 and the mu-opioid receptor in vitro. In vivo,49 displayed potent, dose-dependent antinociceptive activity in both the 1st and 2nd phases in the formalin assay. Consistent with its postulated mechanism, we confirmed that in vivo, as in vitro, compound 49 both antagonized TRPV1 and functioned as a mu-opioid agonist. This result indicates that dual-acting TRPV1 antagonist/mu-opioid ligands can be made and represent a new and promising class of analgesic.

100 Deals associated with Compound 49(Seoul National University)

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