Delving into the Latest Updates on AT-004 (Arctic Therapeutics) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Mechanism-

Therapeutic Areas

Immune System DiseasesCongenital DisordersSkin and Musculoskeletal Diseases

Active Indication

Acne VulgarisDermatitis, AtopicPsoriasis+ [1]

Inactive Indication-

Originator Organization

Arctic TherapeuticsStartup

Active Organization

Arctic TherapeuticsStartup

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Nociceptin/Orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP). In this study novel nonpeptide NOP ligands were characterized in vitro in receptor binding and [³⁵S]GTPγS stimulated binding in membranes of cells expressing human NOP and classical opioid receptors, calcium mobilization assay in cells coexpressing the receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, the electrically stimulated mouse vas deferens and the mouse colon bioassays. The action of the AT compounds were compared with standard NOP agonists (N/OFQ and Ro 65-6570) and the NOP selective antagonist SB-612111. AT compounds displayed high NOP affinity and behaved as NOP agonists in all the functional assays consistently showing the following rank order of potency AT-127≥AT-090≥AT-035>AT-004= AT-001. AT compounds behaved as NOP full agonists in the calcium mobilization and mouse colon assays and as partial agonists in the [³⁵S]GTPγS and BRET assays. Interestingly AT-090 and AT-127, contrary to standard nonpeptide agonists that display G protein biased agonism, behaved as an unbiased agonists. AT-090 and AT-127 displayed higher NOP selectivity than Ro 65-6570 at native mouse receptors. AT-090 and AT-127 might be useful pharmacological tools for investigating the therapeutic potential of NOP partial agonists.

100 Deals associated with AT-004 (Arctic Therapeutics)

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acne Vulgaris	Phase 2	US	Arctic TherapeuticsStartup	-
Dermatitis, Atopic	Phase 2	US	Arctic TherapeuticsStartup	-
Psoriasis	Phase 2	US	Arctic TherapeuticsStartup	-
Rosacea	Phase 2	US	Arctic TherapeuticsStartup	-