Drug intelligence / Profile preview

5-(n,n-dimethyl)amiloride hydrochloride

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
01

Overview

**5-(N,N-dimethyl)amiloride hydrochloride** is a small molecule inhibitor of Na+/H+ exchangers (notably the NHE family, such as SLC9A1/NHE1), which are membrane transport proteins that regulate intracellular pH by exchanging intracellular H+ for extracellular Na+[1][4][5][6][8]. By blocking these exchangers, this molecule decreases intracellular pH and can inhibit pH-dependent cellular processes. It also weakly blocks the transient receptor potential ankyrin 1 (TRPA1) channel (IC50 = 80 µM)[4]. The compound is a derivative of amiloride, originally developed as a research tool, and is used widely in laboratory settings for studying ion transport, ischemia, cell volume regulation, and pain signaling[1][4][5][6][8]. 5-(N,N-dimethyl)amiloride hydrochloride is not approved for clinical or veterinary use and is available only as a research chemical.

Other names
dimethylamiloride hydrochloride5-dimethylamiloride5-(n,n-dimethyl)-amiloride3-amino-6-chloro-n-(diaminomethylene)-5-(dimethylamino)pyrazinamide3-amino-n-carbamimidoyl-6-chloro-5-(dimethylamino)pyrazine-2-carboxamideDMA hydrochlorideamiloride 5-(n,n-dimethyl)- hydrochloride3-amino-6-chloro-n-(diaminomethylidene)-5-(dimethylamino)pyrazine-2-carboxamide
02

Targets

NHE3 (Sodium/hydrogen exchanger 3)NHE1 (Sodium/hydrogen exchanger 1)NHE2 (Sodium-hydrogen exchanger 2)TRPA1 (Transient receptor potential cation channel subfamily A member 1)

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