Amiloride HCl dihydrate

Names

[ Name ]:
Amiloride HCl dihydrate

[Synonym ]:
Modamide
Amiloride hydrochloride dihydrate
AMILORIDEHYDROCHLORIDE,USP
UNII-FZJ37245UC
3,5-Diamino-N-carbamimidoyl-6-chloro-2-pyrazinecarboxamide hydrochloride dihydrate
Midamor
Miloride hydrochloride dihydrate
AMILORIDE HYDROCHLORIDE 2-HYDRATE
2-Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, hydrochloride, hydrate (1:1:2)
AMILORIDE HCL DIHYDRATE

Biological Activity

[Description]:

Amiloride hydrochloride dihydrate is an inhibitor of both Epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA).

[Related Catalog]:

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

Research Areas >> Neurological Disease

[Target]

ENaC[1], uTPA[2]

[In Vivo]

Amiloride hydrochloride dihydrate is a potent epithelial sodium channels (ENaCs) blocker. Amiloride is highly concentrated in the plasma 15 to 30 minutes following the injections. 2 mg/kg dose of Amiloride hydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, or hindquarters vascular resistance as compare to the baseline measurements (n=7). Over a 2 hour period, Amiloride hydrochloride dihydrate elicits negligible responses in arterial pressure (-1±1 mmHg) and heart rate (-10±6 bpm/min) as compare to baseline levels. Results show an Amiloride hydrochloride dihydrate dose-related response pattern for the c-Fos activation in the area postrema (AP). Even at the lowest dose of Amiloride hydrochloride dihydrate (0.1 mg/kg), the number of c-Fos labeled neurons in the AP is statistically different from the control rats at a p<0.01 level[1].

[Animal admin]

The experiments are performed on male and female Sprague-Dawley rats that have been maintained in a heat controlled room maintained at 23° C with a 12h/12h light-dark schedule. A total of 116 adult rats are injected i.p. with Amiloride hydrochloride dihydrate (0.1, 0.5, and 2.0 mg/kg). After 15, 30, 45, or 120 min post-injection, the rats are anesthetized with 8% chloral hydrate, the chest is opened, and blood samples are obtained by cardiac puncture. The blood is centrifuged at 5000 RPM for 5 min, and the plasma (1.5 mL) separated and stored at -80° C[1].

[References]

[1]. Miller RL, et al. Blockade of ENaCs by amiloride induces c-Fos activation of the area postrema. Brain Res. 2015 Mar 19;1601:40-51.

[2]. Xu LB, et al. Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet Mol Res. 2015 Aug 14;14(3):9518-29.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
628.1ºC at 760 mmHg

[ Melting Point ]:
>240℃

[ Molecular Formula ]:
C₆H₁₃Cl₂N₇O₃

[ Molecular Weight ]:
302.118

[ Flash Point ]:
333.7ºC

[ Exact Mass ]:
301.045685

[ PSA ]:
175.25000

[ LogP ]:
1.94440

[ Vapour Pressure ]:
1.08E-15mmHg at 25°C

[ Storage condition ]:
-20°C

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933599090

Customs

[ HS Code ]: 2933599090

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Related Compounds

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