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 D4.4 receptor and Gαqo5. 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).
Uses
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].
References
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[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.
