Drug intelligence / Profile preview

AR-R17779

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Subcutaneous
01

Overview

AR-R17779 is a potent, selective, and blood–brain barrier-penetrant full agonist of the α7 subtype of neural nicotinic acetylcholine receptors (CHRNA7). It acts as a conformationally restricted analog of acetylcholine, displaying high specificity for CHRNA7 with low cross-reactivity for other receptors, such as 5-HT3. In animal studies, AR-R17779 demonstrates nootropic (cognitive-enhancing) effects, can improve learning and memory performance (including reversing working memory deficits), and modulates immune cell populations. Therapeutic investigations include neuroprotection, inflammation, arthritis, and oncology, especially where α7 nAChR signaling can modulate immune and neural responses.

02

Targets

CHRNA7 (α7 nicotinic receptor)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)HTR3A (5-hydroxytryptamine receptor 3A)

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