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MIDD0301

Catalog No. T9946   CAS 2187489-08-1

MIDD0301 is a potent positive allosteric α5β3γ selective GABAA receptor (GABAAR) ligand with EC50 of 17 nM.

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MIDD0301 Chemical Structure
MIDD0301, CAS 2187489-08-1
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MIDD0301 is a potent positive allosteric α5β3γ selective GABAA receptor (GABAAR) ligand with EC50 of 17 nM.
In vivo MIDD0301 did not reveal signs of general toxicity as determined by animal weight, organ weight or haematology after employing oral administration of mice twice daily with 100 mg/kg MIDD0301 mixed in peanut butter for 28 days [1]. Spleen and thymus weights were unchanged and the number of small intestine Peyer's patches was not affected in MIDD0301-treated mice.MIDD0301 treatment did not alter IgG antibody responses to dinitrophenyl following dinitrophenyl-keyhole limpet haemocyanin immunization [1]. MIDD0301 relaxed histamine-contracted guinea pig ( P < 0.05, n = 6-9) and human ( P < 0.05, n = 6-10) tracheal smooth muscle ex vivo in organ bath experiments, dilates mouse peripheral airways ex vivo in precision-cut lung-slice experiments ( P < 0.001, n = 16 airways from three mice), and alleviates bronchoconstriction in vivo in mice, as assessed by the forced-oscillation technique ( P < 0.05, n = 6 mice) [2].
Molecular Weight 414.23
Formula C19H13BrFN3O2
CAS No. 2187489-08-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Nicolas M Zahn, et al. MIDD0301 - A first-in-class anti-inflammatory asthma drug targets GABA A receptors without causing systemic immune suppression. Basic Clin Pharmacol Toxicol. 2019 Jul;125(1):75-84. 2. Gene T Yocum, et al. A novel GABA A receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo. Am J Physiol Lung Cell Mol Physiol. 2019 Feb 1;316(2):L385-L390.

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Keywords

MIDD0301 2187489-08-1 Membrane transporter/Ion channel Neuroscience GABA Receptor MIDD-0301 MIDD 0301 inhibitor inhibit

 

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