- Alomone Labs Clobenpropit dihydrobromide inhibits NMDA receptor channels expressed in Xenopus oocytes.A. Representative time course of NR1/NR2A currents, elicited by transient stimulations with 100 µM glutamate + 100 µM glycine every 50 sec, while membrane potential was held at -80 mV, and reversibly inhibited by 5 µM Clobenpropit dihydrobromide (#C-345). B. Superimposed current traces from the recording shown in A, after application of control and 5 µM Clobenpropit dihydrobromide, as indicated. Transient stimulation is indicated by the arrow.
Clobenpropit dihydrobromide (VUF 9153) is a synthetic compound that acts as a potent, selective and competitive antagonist of the histamine H3 receptor and shows partial agonist activity towards the histamine H4 receptor. In addition, the compound acts as an antagonist of N-Methyl-d-aspartate (NMDA) receptors1 and displays IC50 values of 1 µM-14 µM2.
NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play an important role in a variety of cellular processes and brain functions such as, synaptic plasticity, addiction and stroke, and mediate physiological functions such as learning and memory formation and participates in glutamate excitotoxicity2.
Histamine H3 receptors are presynaptic G-protein coupled receptors that are expressed in the central nervous system. They regulate the release of several neurotransmitters, including biogenic amines, acetylcholine, GABA and glutamate3.
Clobenpropit dihydrobromide (#C-345) is a highly pure, synthetic, and biologically active compound.