Delving into the Latest Updates on DBO-83 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

nAChRs

Mechanism

Nicotinic receptors agonists

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Cognition DisordersPain

Originator Organization

University of Florence

Active Organization-

Inactive Organization

University of Florence

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC10H15Cl3N4

InChIKeyFMBGHZXNKMHVDT-UHFFFAOYSA-N

CAS Registry195211-53-1

Due to the limitations of currently available analgesics, a number of novel alternatives are currently under investigation, including neuronal nicotinic acetylcholine receptor (nAChR) agonists. During the 1990s, the discovery of the antinociceptive properties of the potent nAChR agonist epibatidine in rodents sparked interest in the analgesic potential of this class of compounds. Although epibatidine also has several mechanism-related toxicities, the identification of considerable nAChR diversity suggested that the toxicities and therapeutic actions of the compound might be mediated by distinct receptor subtypes. Consistent with this view, a number of novel nAChR agonists with antinociceptive activity and improved safety profiles in preclinical models have now been identified, including A-85380, ABT-594, DBO-83, SIB-1663 and RJR-2403. Of these, ABT-594 is the most advanced and is currently in Phase II clinical evaluation. Nicotinically-mediated antinociception has been demonstrated in a variety of rodent pain models and is likely mediated by the activation of descending inhibitory pathways originating in the brainstem with the predominant high-affinity nicotine site in brain, the alpha4beta2 subtype, playing a critical role. Thus, preclinical findings suggest that nAChR agonists have the potential to be highly efficacious treatments in a variety of pain states. However, clinical proof-of-principle studies will be required to determine if nAChR agonists are active in pathological pain.

100 Deals associated with DBO-83

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