Overview

Cat #: P-155

Lyophilized Powder yes

Source Synthetic

MW: 592.7

Purity: >99%

Effective concentration 100 nM - 5 µM.

Structure

Chemical name 1,5-Bis(p-amidinophenoxy)pentane bis(2-hydroxyethanesulfonate salt).

Molecular formula C₂₃H₃₆N₄O₁₀S₂.

CAS No.: 140-64-7

PubChem CID 8813

Activity Pentamidine is an uncompetitive NMDA receptor antagonist. It is neuroprotective and inhibits constitutive nitric oxide synthase in the brain. IC₅₀ = 0.72 μM (NR2A), 1.5 μM (NR2B), 10 μM (NR2C), 9.1 μM (NR2D)¹.

References-Activity

Reynolds, I.J. and Aizenman, E. (1992) J. Neurosci. 12, 970.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility 50 mM in H₂O. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs Pentamidine isethionate salt inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes.
A. Time course of NMDA currents that were elicited by stimulation with 10 µM glutamate co-applied with 10 µM glycine every 50 sec, while membrane potential was held at -80 mV. 1 and 10 µM Pentamidine isethionate salt (#P-155), applied for 4 min each, as indicated, reversibly inhibited current amplitude. B. Superimposed current traces taken from the experiment described in A.

References - Scientific background

Reynolds, I.J. and Aizenman, E. (1992) J. Neurosci. 12, 970.
Kaur, G. and Rajput, B. (2014) J. Parasitol. Res. 2014, 726328.
Esposito, G. et al. (2012) J. Neuroinflammation 9, 277.

Scientific background

Pentamidine, an aromatic diamidine, is a potent and effective NMDA receptor antagonist. It has the ability to protect neurons and to prevent the lethal neurotoxic effects actions of NMDA exposure in vitro in primary cultures of cortical neurons and has an antiprotozoal activity.

Pentamidine is being clinically used for prophylaxis and treatment of Pneumocystis carinii pneumonia in patients with AIDS. NMDA antagonists may be therapeutically useful for AIDS patients in order to prevent or delay the onset of the component of dementia that appears from the loss of neurons¹.

In addition, Pentamidine also inhibits the activity of S-adenosyl-L-methionine decarboxylase enzyme, interferes with polyamine synthesis, and decreases mitochondrial membrane potential. The main target for the drug seems to be parasitic mitochondria. Pentamidine is also being used as an alternative treatment for Visceral Leishmaniasis².

Intestinal inflammation can be driven by enteroglial-derived S100B protein. pentamidine has been reported to inhibit S100B activity because of its ability to block the interaction at the Ca²⁺/p53 site of the protein. Pentamidine shows anti-inflammatory effect of acute colitis in a mouse model, likely targeting S100B activity. Pentamidine might be used as pharmacological tool against colitis³.

Target NMDA receptors

Lyophilized Powder

Certificate of Analysis

Pentamidine isethionate salt (#P-155) is a highly pure, synthetic, and biologically active compound.

Order Summary

Pentamidine isethionate salt

Overview

Applications

Citations

Specifications

Scientific Background

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