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

L-745870 hydrochloride 

Cat. No.: HY-14325B Purity: 99.88%
Handling Instructions

L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 hydrochloride has excellent brain penetration.

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

L-745870 hydrochloride Chemical Structure

L-745870 hydrochloride Chemical Structure

CAS No. : 1173023-36-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 82 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of L-745870 hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 hydrochloride has excellent brain penetration[1][2][3].

IC50 & Target

Ki: 0.43 nM (Human dopamine D4 receptor), 960 nM (Human dopamine D2 receptor), 2300 nM (Human dopamine D3 receptor)[1][3]

In Vitro

In vitro pharmacological studies revealed that L-745870 is an antagonist at human D4 receptors, in that 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][2].

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[2].
Evaluation of L-745870 in surrogate marker assays demonstrates that this compound is freely available for biological activity in the brain and that at doses of 5 to 60 mg/kg p.o. L-745870 would occupy 50% D4 receptors in the brain. L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100 mg/kg p.o. that is likely to occupy D2 receptors in vivo. High doses of L-745870 might also be expected to cause extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors. 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][2].

Molecular Weight

363.28

Formula

C₁₈H₂₀Cl₂N₄

CAS No.

1173023-36-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

L-745870L745870L 745870Dopamine ReceptorHumandopamineD4receptorbrainpenetrationneurolepticsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
L-745870 hydrochloride
Cat. No.:
HY-14325B
Quantity:
MCE Japan Authorized Agent: