| Description | BZAD01 is a selective NMDA NR1A/2B receptor antagonist. |
| In vivo | Parkinsonism was induced by microinjection of the toxin, 6-hydroxydopamine (6-OHDA) into the medial forebrain bundle (MFB) of 40 Sprague-Dawley rats. Parkinsonism and the efficacy of drugs were assessed using a battery of behavioural tests including balance beam, apomorphine-induced rotation, body axis bias or "curling", head position bias and disengage sensorimotor latency test. The main effects were that BZAD01 co-administration prevented chronic levodopa-induced potentiation of apomorphine rotation. However levodopa-treated rats were slower than either controls or BZAD-01-treated rats in the locomotor test[2]. |
| Synonyms | BZAD-01, BZAD 01 |
| molecular weight | 362.27 |
| Molecular formula | C16H12F6N2O |
| CAS | 305339-41-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/ml (151.82 mM) |
| References | 1. Beinat C, et al. Structure-activity relationships of N-substituted 4-(trifluoromethoxy)benzamidines with affinity for GluN2B-containing NMDA receptors. Bioorg Med Chem Lett. 2014 Feb 1;24(3):828-30. 2. Warraich ST, et al. Evaluation of behavioural effects of a selective NMDA NR1A/2B receptor antagonist in the unilateral 6-OHDA lesion rat model. Brain Res Bull. 2009 Feb 16;78(2-3):85-90. 3. Leaver KR, et al. Neuroprotective effects of a selective N-methyl-D-aspartate NR2B receptor antagonist in the 6-hydroxydopamine rat model of Parkinson's disease. Clin Exp Pharmacol Physiol. 2008 Nov;35(11):1388-94. |