Sigma-Aldrich L-745,870 Trihydrochloride

Assay

≥99% (HPLC)

Quality Level

100

Form

solid

Potency

0.4 nM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

water: soluble

Storage Temp.

2-8°C

Inchi

1S/C18H19ClN4/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18/h1-7,12H,8-11,13H2,(H,20,21)

General Description

Selective D₄receptor antagonist with excellent brain penetration. Displays an affinity (K_i) of 0.4 nM for human D₄receptors with >1000-fold binding selectivity over D₂and D₃receptors. Does not block agonist-induced activation of GIRK currents. It is used frequently in retinal and CNS studies of D₄modulation.

Biochem/Physiol Actions

Primary Target
D₄Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Li, H. et al., 2013.J. Neurosci. 33,3135.

Pillai, G. et al. 1998.Neuropharmacol. 337,983.
Kulagowski, J. et al. 1996.J. Med. Chem. 39,1941.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany