L-745870

Antagonist of DRD4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe L-745870 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

DRD4

Antagonist

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Within Target family: Selective against human D2 and D3 receptors with Ki 960 and 2300 nM respectively. Outside Target family: Interaction of L-745870 with human and mammalian neurotransmitter receptors was assessed not highlighting any relevant activity. (PMID: 9353380)

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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.

(last updated: 25 Jul 2022 )

SERP Ratings

In Model Organisms

(last updated: 2 Aug 2022 )