5-(N,N-Hexamethylene)amiloride

5-(N,N-Hexamethylene)amiloride is a derivative of the diuretic drug amiloride, which is primarily known for its role as a potassium-sparing diuretic. This compound is of interest in the field of pharmacology due to its ability to inhibit certain ion channels and transporters, particularly the sodium-hydrogen exchanger (NHE).

Chemical Structure and Properties

5-(N,N-Hexamethylene)amiloride is a modified version of amiloride, where the pyrazine ring is substituted with a hexamethylene group. This modification alters its pharmacokinetic and pharmacodynamic properties, potentially enhancing its specificity and potency against certain targets.

Molecular Formula

The molecular formula of 5-(N,N-Hexamethylene)amiloride is C₁₂H₁₈N₄O.

Molecular Weight

The molecular weight of this compound is approximately 234.3 g/mol.

Mechanism of Action

5-(N,N-Hexamethylene)amiloride functions primarily as an inhibitor of the sodium-hydrogen exchanger (NHE), a membrane protein that plays a critical role in regulating intracellular pH and cell volume. By inhibiting NHE, this compound can affect various physiological processes, including cell proliferation, migration, and apoptosis.

Pharmacological Effects

The pharmacological effects of 5-(N,N-Hexamethylene)amiloride are largely attributed to its ability to modulate ion transport across cell membranes. This can lead to changes in cellular homeostasis and has potential therapeutic implications in conditions such as hypertension, heart failure, and certain types of cancer.

Research and Clinical Applications

Research into 5-(N,N-Hexamethylene)amiloride has focused on its potential use in treating diseases characterized by dysregulated ion transport. Studies have explored its effects in models of cardiovascular disease, cancer, and other conditions where NHE activity is implicated.

Safety and Toxicity

As with any pharmacological agent, the safety and toxicity profile of 5-(N,N-Hexamethylene)amiloride must be thoroughly evaluated. Preclinical studies are necessary to assess its potential side effects and therapeutic window.

Also see

• Amiloride
• Sodium-hydrogen exchanger
• Diuretics
• Ion channels
• Pharmacology