Cariprazine is a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Cariprazine exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM). Cariprazine has lower affinity at human and rat hippocampal 5-HT1A receptors (pKi 8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Administration of Cariprazine (30 µg/kg) reduces the striatal uptake of both radioligands to the level of nonspecific binding compared with baseline PET measurements.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 10 mM|
Cariprazine Exerts Antimanic Properties and Interferes With Dopamine D2 Receptor β-arrestin Interactions
Yonglin Gao, et al. Pharmacol Res Perspect. 2015 Feb;3(1):e00073. PMID: 25692006.
Occupancy of Dopamine D₂ and D₃ and Serotonin 5-HT₁A Receptors by the Novel Antipsychotic Drug Candidate, Cariprazine (RGH-188), in Monkey Brain Measured Using Positron Emission Tomography
Nicholas Seneca, et al. Psychopharmacology (Berl). 2011 Dec;218(3):579-87. PMID: 21625907.
Cariprazine (RGH-188), a Dopamine D(3) Receptor-Preferring, D(3)/D(2) Dopamine Receptor Antagonist-Partial Agonist Antipsychotic Candidate: In Vitro and Neurochemical Profile
Bela Kiss, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40. PMID: 20093397.
|Related Dopamine Receptor Products|
ML417 is a highly selective and brain penetrant D3 dopamine receptor (D3R) agonist, with EC50 of 38 nM.
PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively.
SCH23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively).
MPTP hcl is a compound to the neurotoxin MPP+ which causes permanent symptoms of Parkinson's disease.
SKF38393 HCl is a selective D1 dopamine receptor agonist with IC50 of 110 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.