4-Amino-5-chloro-N-(1-((4-fluorophenyl)methyl)-4-piperidinyl)-2-methox ybenzamide Chemical Properties

Boiling point:

518.2±50.0 °C(Predicted)

Density 

1.31±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml

form 

A crystalline solid

pka

13.62±0.20(Predicted)

color 

White to off-white

4-Amino-5-chloro-N-(1-((4-fluorophenyl)methyl)-4-piperidinyl)-2-methox ybenzamide Usage And Synthesis

Description

Fluoroclebopride is a benzamide analog that is used in positron emission tomography (PET) applications. It binds reversibly to dopamine receptors (K_is = 0.95, 5.7, 5.46, and 144 nM for D₂-like, D_2(long), D₃, and D₄ receptors, respectively, in radioligand binding assays). It is selective for these receptors over D₁, serotonin 5-HT₂, and α₂-adrenergic receptors (K_is = >10,000, 283, and 1,300 nM, respectively). A fluorine-18 moiety has been used to label this compound for use as a probe for studying D₂/D₃ receptor availability via PET in various monkey models.

Uses

Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models[1][2].

References

[1] Nader MA, Czoty PW. PET imaging of dopamine D2 receptors in monkey models of cocaine abuse: genetic predisposition versus environmental modulation. Am J Psychiatry. 2005 Aug;162(8):1473-82. DOI:10.1176/appi.ajp.162.8.1473
[2] Czoty PW, et al. Effects of repeated treatment with the dopamine D2/D3 receptor partial agonist aripiprazole on striatal D2/D3 receptor availability in monkeys. Psychopharmacology (Berl). 2013 Sep 29:10.1007/s00213-013-3274-7. DOI:10.1007/s00213-013-3274-7. doi: 10.1007/s00213-013-3274-7