Inhibitors Product Data Sheet
Bifemelane hydrochloride • Agonists
Cat. No.: HY-B1558A CAS No.: 62232-46-6
Molecular Formula: C₁₈H₂₄ClNO •
Molecular Weight: 305.84 Screening Libraries Target: Monoamine Oxidase Pathway: Neuronal Signaling Storage: 4°C, protect from light * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
SOLVENT & SOLUBILITY
In Vitro DMSO : 250 mg/mL (817.42 mM; Need ultrasonic)
Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 3.2697 mL 16.3484 mL 32.6968 mL Stock Solutions 5 mM 0.6539 mL 3.2697 mL 6.5394 mL
10 mM 0.3270 mL 1.6348 mL 3.2697 mL
Please refer to the solubility information to select the appropriate solvent.
In Vivo 1. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.08 mg/mL (6.80 mM); Clear solution
2. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08 mg/mL (6.80 mM); Clear solution
3. Add each solvent one by one: 10% DMSO >> 90% corn oil Solubility: ≥ 2.08 mg/mL (6.80 mM); Clear solution
BIOLOGICAL ACTIVITY
Description Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with
a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease[1][2].
IC₅₀ & Target MAO-A MAO-B 4.2 μM (Ki) 46 μM (Ki)
In Vitro Bifemelane inhibits MAO-A in a dose-dependent manner, with Kis of 4.2±0.2 and 14.1±0.7 μM in human brain synaptosomes
Page 1 of 2 www.MedChemExpress.com and human liver mitochondria respectively[1].
Bifemelane inhibits MAO-B activities in a dose-dependent manner, with Kis of 46.0±3.6 and 65.2±7.0 μM in human brain synaptosomes and human liver mitochondria respectively[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo Bifemelane (20-80 mg/kg; i.p.) dose-dependently decreases exploratory activity in the open field test[3]. Bifemelane (20-80 mg/kg; i.p.) decreases immobility time in the forced swim test, although is not clearly dosedependent and has already reached ceiling at 20 mg/kg[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Wistar male rats (230-270 g) are induced hypothermia by Reserpine[3]
Dosage: 20, 40, 80 mg/kg
Administration: A single i.p.
Result: Attenuated the Reserpine-induced hypothermia by a maximum of 10 .
REFERENCES
[1]. Naoi M, et, al. 4-(O-benzylphenoxy)-N-methylbutylamine (bifemelane) and other 4-(O-benzylphenoxy)-N-methylalkylamines as new inhibitors of type A and B monoamine oxidase. J Neurochem. 1988 Jan; 50(1): 243-7.
[2]. Fasipe OJ, et, al. The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. IBRO Rep. 2019 Jan 9; 6:95-110.
[3]. Moryl E, et, al. Potential antidepressive properties of amantadine, memantine and bifemelane. Pharmacol Toxicol. 1993 Jun; 72(6): 394-7.
McePdfHeight
Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Page 2 of 2 www.MedChemExpress.com