2-[[4-(2-Pyridinyl)-1-piperazinyl]Methyl]-1H-benziMidazole trihydrochloride

Description

ABT-724 is a dopamine D₄ receptor agonist with an EC₅₀ value of 12.4 nM in a FLIPR calcium flux assay using HEK293 cells expressing the human D_4.4 receptor and Gα_qo5. It is selective for dopamine D₄ over D₂ receptors at 10 μM. ABT-724 (0.03 μmol/kg) induces penile erections in 77% of male rats. It decreases mounting frequency and ejaculation latency and increases ejaculation frequency and copulatory efficacy in male rats when administered at a dose of 0.04 mg/kg. ABT-724 (0.16 and 0.64 mg/kg) decreases hyperactivity and exploratory behavior in the open field test in an adolescent spontaneously hypertensive rat (SHR) model of attention-deficit hyperactivity disorder (ADHD).

storage

+4°C (desiccate)

References

[1]. sarkar c, das s, chakroborty d, et al. cutting edge: stimulation of dopamine d4 receptors induce t cell quiescence by up-regulating kruppel-like factor-2 expression through inhibition of erk1/erk2 phosphorylation. j immunol, 2006, 177(11):7525-9.
[2]. melis mr, succu s, mascia ms, et al. pd-168077, a selective dopamine d4 receptor agonist, induces penile erection when injected into the paraventricular nucleus of male rats. neurosci lett, 2005, 379(1):59-62.
[3]. sanna f, contini a, melis mr, et al. role of dopamine d4 receptors in copulatory behavior: studies with selective d4 agonists and antagonists in male rats. pharmacol biochem behav, 2015, 137:110-8.
[4]. arranz m, collier d, sodhi m, et al. association between clozapine response and allelic variation in 5-ht2a receptor gene. lancet, 1995, 346(8970):281-2.
[5]. boehmler w, carr t, thisse c, et al. d4 dopamine receptor genes of zebrafish and effects of the antipsychotic clozapine on larval swimming behaviour. genes brain behav, 2007, 6(2):155-66.

Raw materials

Preparation Products