1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Rilmazafone hydrochloride

Rilmazafone hydrochloride  (Synonyms: 450191S)

Cat. No.: HY-U00228 Purity: 99.75%
COA Handling Instructions

Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand.

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

Rilmazafone hydrochloride Chemical Structure

Rilmazafone hydrochloride Chemical Structure

CAS No. : 85815-37-8

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Description

Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand[1].

In Vivo

When the animals are pretreated with high doses of Rilmazafone hydrochloride (450191-S; 200 or 600 mg/kg for 5 or 3 days, respectively) to induce hepatic drug-metabolizing enzymes, plasma concentrations of the metabolites after oral administration of a dose of 200 mg/kg of Rilmazafone decrease markedly depending on the induced enzyme activity. Pretreatment of rats with phenobarbital also causes decreased plasma levels of metabolites, which are almost the same as those in Rilmazafone-pretreatment. On the other hand, administration of beta-naphthoflavone to rats leads to higher plasma levels of metabolites, and slower elimination compared with those in the control and Rilmazafone or Phenobarbital pretreated rats. Rilmazafone is demonstrated to stimulate the hepatic drug-metabolizing enzymes in rats, mice and dogs, which is accompanied by a marked reduction in the pharmacological activity of pentobarbital in rats. The induction of hepatic enzyme activities by Rilmazafone is detected only when the plasma concentrations of its metabolites are very high[2].

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

Molecular Weight

511.79

Formula

C21H21Cl3N6O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NCC(NCC1=NC(C(N(C)C)=O)=NN1C2=C(C=C(Cl)C=C2)C(C3=C(C=CC=C3)Cl)=O)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (488.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9539 mL 9.7696 mL 19.5393 mL
5 mM 0.3908 mL 1.9539 mL 3.9079 mL
10 mM 0.1954 mL 0.9770 mL 1.9539 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
Animal Administration
[2]

Mice[2]
Adult male rats of the Jcl Sprague-Dawley strain, 7-8 weeks old, are used for the experiments. The animals are kept in an air-conditioned room (25±1°C, 50-60% humidity) lighted 12 hr a day (8:00-20:00) and maintain on com mercial rat chow and water ad libitum. Rilmazafone is dissolved in 5% (w/v) arabic gum at 20 or 60 mg/mL, and the resulting solution is administered orally to rats at 1.0 mL/100 g body weight for 3-5 days. Typical inducers, phenobarbital (in physiological saline) and beta-naphthoflavone (in sesame oil), are administered intraperitoneally at a dose of 40 mg/kg, once daily for 3 days. The animals are fasted for 24 hr after the last adminis tration of Rilmazafone or inducers, and then the test solution of Rilmazafone (20 mg/mL of 5% arabic gum) is given orally to rats at a dose of 200 mg/kg. Heparinized blood samples are obtained from the abdominal aorta under ether anesthesia and centrifuged immediately to obtain plasma samples using an Eppendorf centrifuge Type 5414S.

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

References
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Rilmazafone hydrochloride Related Classifications

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Rilmazafone hydrochloride
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