Cartazolate

Cartazolate (SQ 65396) enhances the binding of ³H-diazepam to crude P₂ membrane fragments from rat frontal cortex by increasing ligand affinity (reducing K_d from 5.27 nM to 2.45 nM at a concentration of 1 μM), without altering the number of binding sites^[1].
Cartazolate (0.3-1000 μM; 30 min) reversibly stimulates Na⁺-independent ³H-GABA binding to rat frontoparietal cortical membranes in vitro, with a half-maximal effective concentration (EC₅₀) of 3 μM^[2].
Cartazolate (30 μM; 30-40 min) exerts a stimulatory effect on non-Na⁺-dependent ³H-GABA binding to rat frontoparietal cortical membranes, and this regulatory activity is partially dependent on chloride ions: the stimulatory effect maintains baseline levels under chloride-free conditions, is strengthened at moderate chloride concentrations, and is weakened at high chloride concentrations^[2].
Cartazolate (30 μM; 60 min) increases the apparent number of ³H-muscimol binding sites in the cerebral cortex cell membranes of rat frontoparietal cortex in vitro, elevating the B_max from 2.7 pmol/mg protein to 4.2 pmol/mg protein under chloride-free conditions, and to 6.1 pmol/mg protein under 100 mM chloride conditions^[2].
Cartazolate potently stimulates the specific binding of [³H]flunitrazepam to rat cerebellar membranes by increasing the apparent affinity, with an EC₅₀ of 0.3 μM. It sensitizes the rat cerebellar GABA/benzodiazepine receptor complex to GABA, increases the apparent affinity of GABA-stimulated [³H]flunitrazepam binding, and enhances the maximal stimulatory effect of GABA^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.