Istradefylline (KW-6002) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat, 105.02 nM and 1.87 nM for A1 receptor and A2A receptor in mouse, respectively.
Oral administration of Istradefylline improves motor disability in MPTP-treated parkinsonian marmosets in a dose-dependent manner without provoking dyskinesia. Istradefylline treatment potentiates rotational behavior induced by dopaminergic drugs in hemi-Parkinsonian rats. Istradefylline treatment alone causes an approximately 20% reduction in the striatal levels of preproenkephalin mRNA, whereas neither the coadministration of KW-6002 and L-DOPA nor L-DOPA alone significantly alters the expression of this transcript in the dopamine-denervated striatum.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Common marmosets (Callithrix jacchus) with MPTP treatment |
| Formulation | Suspended in 0.3% Tween-80 and 10% sucrose solution |
| Dosages | 10 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 384.43 |
| Formula | C20H24N4O4 |
| CAS Number | 155270-99-8 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
[1] No authors listed. Istradefylline
[5] Thomas Mller. The safety of istradefylline for the treatment of Parkinson's disease
| Related Adenosine Receptor Products |
|---|
| LUF5519
LUF5519 is a ribose-containing adenosine A1 receptor agonist. |
| LUF6258
LUF6258 is a hybrid ortho/allosteric ligand of the adenosine A(1) receptor. |
| A3AR agonist 1
A3AR agonist 1 is an A3AR agonist (Ki: 25.8 nM). |
| A3AR agonist 2
A3AR agonist 2 a selective A3AR agonist (Ki: 22.1 nM). |
| Inupadenant hydrochloride
Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
