NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).

Product information

CAS Number: 204718-47-8

Molecular Weight: 439.52

Formula: C24H23F2N3OS

Chemical Name: 4-(4-fluorophenyl)-5-(2-{4-[(3-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-1,3-thiazole-2-carboxamide

Smiles: NC(=O)C1=NC(C2C=CC(F)=CC=2)=C(CCN2CCC(CC2)=CC2=CC=CC(F)=C2)S1

InChiKey: QESXTNJNPLVEOR-UHFFFAOYSA-N

InChi: InChI=1S/C24H23F2N3OS/c25-19-6-4-18(5-7-19)22-21(31-24(28-22)23(27)30)10-13-29-11-8-16(9-12-29)14-17-2-1-3-20(26)15-17/h1-7,14-15H,8-13H2,(H2,27,30)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED50 = 1.0 mg/kg) than on A9 dopamine neurons (ED50 = 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED50 values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively.

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