Delving into the Latest Updates on AL-38022A with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

5-HT2 receptor

Mechanism

5-HT2 receptor agonists(Serotonin 2 (5-HT2) receptor agonists)

Therapeutic Areas

Eye Diseases

Active Indication

Glaucoma

Inactive Indication-

Originator Organization

Alcon Research Ltd.

Active Organization

Alcon Research Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC13H17N3O

InChIKeyFJRIVFVALIEIOY-VIFPVBQESA-N

CAS Registry478132-11-5

AL-38022A is a novel synthetic serotonergic (5-HT) ligand that exhibited high affinity for each of the 5-HT2 receptor subtypes (Ki100-fold less) affinity for other 5-HT receptors. In addition, AL-38022A displayed a very low affinity for a broad array of other receptors, neurotransmitter transport sites, ion channels, and second messenger elements, making it a relatively selective agent. AL-38022A potently stimulated functional responses via native and cloned rat (EC50 range: 1.9-22.5 nM) and human (EC50 range: 0.5-2.2 nM) 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities and was a full agonist at all 5-HT2 receptor subtypes. The CNS activity of AL-38022A was assessed by evaluating its discriminative stimulus effects in both a rat and a monkey drug discrimination paradigm using DOM as the training drug. AL-38022A fully generalized to the DOM stimulus in each of these studies; in monkeys MDL 100907 antagonized both DOM and AL-38022A. The pharmacological profile of AL-38022A suggests that it could be a useful tool in defining 5-HT2 receptor signaling and receptor characterization where 5-HT may function as a neurotransmitter.

100 Deals associated with AL-38022A

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