A-317567

Names

[ Name ]:
A-317567

[Synonym ]:
A-317567

Biological Activity

[Description]:

A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. A-317567 has antidepressant and antinociception effects[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Neurological Disease

[Target]

IC50: 1.025 μM (Acid-sensing ion channel 3 (ASIC-3))[1]

[In Vitro]

The effects of A-317567 on three distinct types of native ASIC currents evoked in acutely dissociated adult rat dorsal root ganglion (DRG) neurons are studied. A-317567 produces concentration-dependent inhibition of all pH 4.5-evoked ASIC currents with an IC50 ranging between 2 and 30 μM, depending upon the type of ASIC current activated. A-317567 equipotently blocks the sustained phase of ASIC3-like current, a biphasic current akin to cloned ASIC3, which is predominant in DRG[2].

[In Vivo]

A-317567 is fully analgesic effects in the CFA model (ED50 of 17 μmol/kg, i.p., adult male Sprague-Dawley rats). There is no significant effect of A-317567 on the withdrawal latency of the contralateral paw under these conditions[2].

[References]

[1]. Kuduk SD, et al. Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567. ACS Chem Neurosci. 2010 Jan 20;1(1):19-24.

[2]. Dubé GR, et al. Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain. 2005 Sep;117(1-2):88-96.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₃₁N₃

[ Molecular Weight ]:
397.55500

[ Exact Mass ]:
397.25200

[ PSA ]:
53.11000

[ LogP ]:
6.31790

Related Compounds

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