371217-32-2

371217-32-2 structure

Name: A-317567
Chemical Name: 6-(2-(1-isopropyl-2-methyl-1,2,3,4-tetrahydro-7-isoquinolinyl)cyclopropyl)-2-naphthalenecarboximidamide
CAS Number: 371217-32-2
Molecular Formula: C₂₇H₃₁N₃
Molecular Weight: 397.55500
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2018-05-09 20:34:49
Modify Date: 2024-01-10 20:57:49
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].

Name	6-(2-(1-isopropyl-2-methyl-1,2,3,4-tetrahydro-7-isoquinolinyl)cyclopropyl)-2-naphthalenecarboximidamide
Synonyms	A-317567

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.