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Chemical Structure| 1173023-36-3 Chemical Structure| 1173023-36-3

Structure of L-745870 HCl
CAS No.: 1173023-36-3

Chemical Structure| 1173023-36-3

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L-745870 HCl is an effective, selective, blood-brain barrier-permeable, and orally active dopamine D4 receptor antagonist, with a Ki value of 0.43 nM. It has weaker affinity for D2 (Ki = 960 nM) and D3 (Ki = 2300 nM) receptors, and moderate affinity for 5-HT2 receptors, sigma sites, and α-adrenergic receptors.

Synonyms: L-745870 hydrochloride

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Product Details of L-745870 HCl

CAS No. :1173023-36-3
Formula : C18H20Cl2N4
M.W : 363.28
SMILES Code : ClC1=CC=C(N2CCN(CC3=CNC4=NC=CC=C43)CC2)C=C1.[H]Cl
Synonyms :
L-745870 hydrochloride
MDL No. :MFCD01529971
InChI Key :GFFJYISJZJIKAF-UHFFFAOYSA-N
Pubchem ID :11957618

Safety of L-745870 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of L-745870 HCl

GPCR

Isoform Comparison

Biological Activity

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

In Vitro:

Cell Line
Concentration Treated Time Description References
P23H rat RGCs 1μM ~10 minutes To investigate the effects of L-745870 on the light sensitivity of P23H rat RGCs. Results showed that L-745870 increased light sensitivity but had no significant effect on the maximum peak response or dynamic range of RGCs. PLoS One. 2015 Dec 30;10(12):e0146154
Sprague-Dawley rat RGCs 1μM ~10 minutes To investigate the effects of L-745870 on the light sensitivity of Sprague-Dawley rat RGCs. Results showed that L-745870 decreased light sensitivity and reduced the maximum peak response of RGCs. PLoS One. 2015 Dec 30;10(12):e0146154

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Anesthetized rat model Subcutaneous injection 5 and 10 mg/kg Single injection To investigate the effect of D4R antagonist on low-frequency oscillations in the prefrontal cortex and hippocampus. Results showed that D4R antagonist decreased delta power in the prefrontal cortex and increased theta power in the hippocampus. Int J Mol Sci. 2022 Oct 3;23(19):11705
Male Wistar rats Satiated rat model Intra-NAc shell microinjection 0.1 µg Single administration, observed for 60 minutes To investigate the effects of D4R agonist PD-168077 and antagonist L-745870 on sweet solution intake in satiated rats. Results showed that PD-168077 significantly increased sweet solution intake (by 46%), and this effect was reversed by L-745870. Brain Sci. 2024 Oct 30;14(11):1103
Adult male C57BL6/J mice Intermittent binge eating model Intraperitoneal injection 5 mg/kg Administered 30 min before each BET, for 3 BET sessions To evaluate the effect of DRD4 antagonist on binge-like intake, results showed that DRD4 antagonist reduced binge-like intake of PF. Front Behav Neurosci. 2025 Apr 29;19:1572374

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.75mL

0.55mL

0.28mL

13.76mL

2.75mL

1.38mL

27.53mL

5.51mL

2.75mL

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