L-745870
Antagonist of DRD4
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
(last updated: 25 Jul 2022 )
SERP Ratings
(last updated: 2 Aug 2022 )
SERP+ Ratings
SERP+ Comments:
(last updated: 14 Oct 2025 )
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In Cell Rating
In Model Organisms
Careful interpretation from in vivo study by means of this compound would be required because of the limited broader selectivity profiles against other targets. One mg/kg (in rats) could be used in lab experiments as the highest dose, but this dose may show D4-independent pheontypes as shown in JPET 283:636–647, 1997.
In Model Organisms
In Cell Rating
In Model Organisms
L-745870 is a brain penetrant antagonist of dopamine D4 receptor, which demonstrates high potency (Ki = 0.4 nM) against D4 and 2000 and 5000 fold selectivity over D2 and D3 receptors, respectively. L-745870 shows antagonism of the dopamine-mediated inhibition of adenylate cyclase in hD4 CHO cells. Weak activity is observed against sigma binding sites and 5HT2A receptors (Ki 0.13 and 0.2 uM, respectively), exhibited little affinity for potassium, calcium or sodium channels (IC50s 2.5, 9.3, 0.1 uM, respectively) or other receptors although data not shown. The pharmacokinetic profile in rats shows a reasonable plasma half-life (2.1h), good oral bioavailability (66%) at 3 mg/kg (i.v. and p.o) dosing.