1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. RWJ-51204

RWJ-51204 

Cat. No.: HY-19308
Handling Instructions

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

For research use only. We do not sell to patients.

RWJ-51204 Chemical Structure

RWJ-51204 Chemical Structure

CAS No. : 205701-85-5

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Description

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

IC50 & Target

Ki: 0.2-2 nM (GABA(A))[1]

In Vitro

RWJ-51204 binds to receptors in the cerebral cortex, cerebellum, or medulla-spinal cord with Ki ranging from 0.2 to 0.6 nM.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RWJ-51204 is orally active in anxiolytic efficacy tests. WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED50 = 0.04 mg/kg). RWJ-51204 is effective in the conflict test in monkeys (ED50 of approximately 0.5 mg/kg p.o.). RWJ-51204 potently impairs rotarod performance in rats (ED50 = 0.12 mg/kg), and all rats given RWJ-51204 orally at 30 mg/kg exhibit sedation, reduced skeletal muscle tone, and impairment of rotarod performance.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

399.39

Formula

C₂₁H₁₉F₂N₃O₃

CAS No.

205701-85-5

SMILES

O=C(C1=C2N(COCC)C3=CC(F)=CC=C3N2CCC1=O)NC4=CC=CC=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[1]

For each sample, a portion of the membrane fraction containing 0.1 to 0.2 mg of protein is incubated in 2 mL of a 3 mM phosphate-buffered solution containing 0.1 M NaCl and 0.01 to 0.03 μCi of a 3H-labeled ligand [3H]Ro15-4513, [3H]flumazenil. The receptor-ligand binding reaction is allowed to reach equilibrium at an ambient temperature of 21-23°C (30 min) and then the reaction is terminated by vacuum filtration to separate the incubation medium from the biological membranes. The membrane samples are washed to remove unbound ligand. The3H bound to each membrane sample is quantified using liquid scintillation spectrometry.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Adult rats are deprived of water for 48 h and are deprived of food for at least 16 h before testing. After the first 24 h of water deprivation, they are placed in a sound-attenuating chamber for a training period, in which they are allowed 200 licks from a bottle containing tap water. The experiment is performed the next day. Vehicle or compounds are administered orally by gavage, and at specified times after dosing, rats are placed in the chamber and allowed access to tap water. The first lick at the stainless steel sipper tube of a water bottle initiates a 3-min test session in which every 20th lick is punished by a 0.2 s, 0.5 mA shock (root mean square, measured across the electrodes) delivered via the sipper tube. If rats fail to drink within 5 min, the experiment is terminated, and they are evaluated for signs of CNS depression. Rats are not reused in this experiment. The anxiolytic effectiveness of a compound in this assay is determined from the number of rats, at each dose, that receive a number of shocks that is equal to or greater than the calculated 90th percentile of the number of shocks received by approximately 600 vehicle-treated rats. This criterion is eight shocks when rats are tested 1 h after administration and 10 shocks when rats are tested 4 h after administration.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

RWJ-51204RWJ51204RWJ 51204GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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Product Name:
RWJ-51204
Cat. No.:
HY-19308
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