L-745870 trihydrochloride

SKU: orb1305783

Description

L-745870 trihydrochloride is a potent and selective dopamine D4 receptor antagonist with moderate affinity for 5-HT2 receptors, sigma sites, and α-adrenoceptors. It is a valuable research tool for investigating D4 receptor function in neuropsychiatric disorders and has been utilized in both in vitro binding assays and in vivo behavioral studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 866021-03-6
• MW: 436.21
• Purity: 99.94% (May vary between batches)
• Formula: C₁₈H₂₂Cl₄N₄
• SMILES: ClC1=CC=C(C=C1)N2CCN(CC2)CC3=CNC4=C3C=CC=N4.Cl.Cl.Cl
• Target: Adrenergic Receptor,Dopamine Receptor,Sigma receptor,5-HT Receptor
• Solubility: H2O:< 40 mg/mL;DMSO:50 mg/mL (114.62 mM)

Bioactivity

• Target IC50:
  D4 receptor:4.3 nM (Ki)|D3 receptor:2300 nM (Ki)|D2 receptor:960 nM (Ki)
• In Vivo:
  L-745870 has favorable pharmacokinetic properties in both rats and monkeys, and shows excellent brain permeability and a high brain-to-plasma ratio in rats . L-745870 (10 mg/kg p.o.) at 30 mg/kg caused mild sedation and extrapyramidal motor symptoms, especially bradykinesia, following oral administration to squirrel monkeys. Lower doses of L-745870 had no apparent behavioral effects in monkeys .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

brain-penetrant, Antipsychotic, 5HTReceptor, 5HT Receptor, 5-HT2, Adrenergic Receptor, AdrenergicReceptor, D4, D4-receptor, D3, D2, DopamineReceptor, Dopamine Receptor, orally, inhibit, L 745870, L 745870 trihydrochloride, L 745870 Trihydrochloride, Inhibitor, L-745,870, L-745,870 trihydrochloride, L-745,870 Trihydrochloride, L745870, L-745870, L745870 trihydrochloride, L745870 Trihydrochloride, L-745870 trihydrochloride, L-745870 Trihydrochloride, Sigmareceptor, Sigma receptor, α-adrenergic receptor, α-adrenoceptors

Compound Identifiers

PubChem CID

49759035