1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. L-745870 trihydrochloride

L-745870 trihydrochloride 

Cat. No.: HY-14325A
Handling Instructions

L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.

For research use only. We do not sell to patients.

L-745870 trihydrochloride Chemical Structure

L-745870 trihydrochloride Chemical Structure

CAS No. : 866021-03-6

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Description

L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].

IC50 & Target[3]

Human D4 Receptor

4.3 nM (Ki)

D2 Receptor

960 nM (Ki)

D3 Receptor

2300 nM (Ki)

In Vitro

L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells; inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1].

In Vivo

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[1].
Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys[1].

Molecular Weight

436.21

Formula

C₁₈H₂₂Cl₄N₄

CAS No.

866021-03-6

SMILES

ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

L-745870 trihydrochlorideDopamine ReceptorAntipsychoticD4-receptor5-HT2α-adrenoceptorsbrain-penetrantorallyInhibitorinhibitorinhibit

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L-745870 trihydrochloride
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