Bromoacetylalprenololmenthane
Bromoacetylalprenololmenthane (BrAAM) is a competitive, slowly reversible β1-adrenoceptor antagonist with membrane-stabilizing effects. Bromoacetylalprenololmenthane causes parallel or non-parallel rightward shifts of the isoproterenol response curve and reversibly inhibits cardiac stimulatory responses. Bromoacetylalprenololmenthane can be used in studies such as determining the affinity constant of isoproterenol, occupancy-response relationships, and receptor reserve.
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- CAS No.: 76298-89-0
- Formula: C24H37BrN2O3
- Molecular Weight:481.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
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Biological Activity
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Beta-1 adrenergic receptor |
Bromoacetylalprenololmenthane (0.25-2.0 μM) irreversibly blocks β-adrenergic receptors in S49 wild-type lymphoma cells (with a half-blocking concentration of 0.5-1.0 μM) and inhibits hormone-induced receptor internalization in a dose-dependent manner; it reduces the internalization rate by 50%-65% at a concentration of 0.63 μM, and completely prevents internalization at concentrations ≥ 2.0 μM[3].
Bromoacetylalprenololmenthane (0.63 μM) reduces the maximum cumulative level of cAMP via receptor blockade, but does not alter the desensitization kinetics of adenylate cyclase in S49 wild-type lymphoma cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 76298-89-0
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Molecular Weight 481.48
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Formula C24H37BrN2O3
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SMILES
O=C(NC(C)(C)C1CCC(NCC(O)COC=2C=CC=CC2CC=C)(C)CC1)CBr
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Synonyms
BrAAM
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Surman AJ, et al. Alprenolol and bromoacetylalprenololmenthane are competitive slowly reversible antagonists at the beta 1-adrenoceptors of rat left atria. Journal of cardiovascular pharmacology. 1993 Jan;21(1):35-9. [Content Brief]
[2]. Doggrell SA, et al. The effects of bromoacetylalprenololmenthane on the responses to isoprenaline of the left ventricle from normo-, prehyper- and hypertensive rats. Journal of autonomic pharmacology. 1997 Jun;17(3):183-90. [Content Brief]
[3]. Box RJ, et al. Bromoacetylalprenololmenthane binding to beta-receptors modulates the rate of hormone-induced internalization but not desensitization in S49 cells. FEBS letters. 1987 Apr 20;214(2):323-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)