NRA-0160
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).
For research use only. We do not sell to patients.
- CAS No.: 204718-47-8
- Formula: C24H23F2N3OS
- Molecular Weight:439.52
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Dopamine Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
MoreAll Adrenergic Receptor Isoforms
More
Biological Activity
|
5-HT2A Receptor |
D4 Receptor 0.48 nM (Ki) |
D3 Receptor 39 nM (Ki) |
5-HT2A Receptor 180 nM (Ki, in rat) |
Rat α1 adrenoceptor 237 nM (Ki) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 204718-47-8
-
Molecular Weight 439.52
-
Formula C24H23F2N3OS
-
SMILES
O=C(C1=NC(C2=CC=C(F)C=C2)=C(CCN3CC/C(CC3)=C\C4=CC=CC(F)=C4)S1)N
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
Methamphetamine (MAP, 1 mg/kg, iv) or apomorphine (APO, 40 μg/kg iv.) and incremental doses of NRA0160 or G745870 (the starting dose is 0.1 mg/kg with sequential doses of 0.2, 0.7 and 2 mg/kg) are administered every 2-3 min (drug-induced changes usually reached their plateaus in 2-3 min) via an i.v. catheter implanted in the femoral vein of rats. Drug-induced changes (after reaching plateau) in neuronal activities which are plotted as percent changes from the preinjection baseline rate, are recorded over a 5 min period and defined as 100%. The % inhibition is calculated and ED50 values are determined. The ED50 values are analyzed by fitting it to the four parametric logistic functions, using non-linear least square regression (-) Apomorphine hydrochloride, methamphetamine HCl and L 745870 3HCl are dissolved in 0.9% saline with the addition of 0.1% ascorbic acid for apomorphine. NRA0160 is dissolved in a minimal amount of 0.5N HCl and distilled water for injection, then titrated is with 0.5N NaOH to a final pH of 5.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[1]. Abekawa T, et al. Effects of NRA0045, a novel potent antagonist at dopamine D4, 5-HT2A, and alpha1 adrenaline receptors, and NRA0160, a selective D4 receptor antagonist, on phencyclidine-induced behavior and glutamate release in rats. Psychopharmacology (Berl). 2003 Sep;169(3-4):247-56. Epub 2003 Jul 31. [Content Brief]
[2]. Kawashima N, et al. Effects of selective dopamine D4 receptor blockers, NRA0160 and L-745,870, on A9 and A10 dopamine neurons in rats. Life Sci. 1999;65(24):2561-71. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)