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About This Item
Empirical Formula (Hill Notation):
C16H21NO2 · xHCl
CAS Number:
Molecular Weight:
259.34 (free base basis)
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze
Quality Segment
assay
≥97% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
methanol: soluble, water: soluble
shipped in
ambient
storage temp.
−20°C
InChI
1S/C17H23NO2.ClH/c1-13(2)10-18-11-15(19)12-20-17-9-5-7-14-6-3-4-8-16(14)17;/h3-9,13,15,18-19H,10-12H2,1-2H3;1H
InChI key
RTTYPFXTLKDXPS-UHFFFAOYSA-N
General description
A highly lipophilic agent that blocks both β1 and β2 adrenergic receptors with equal potency. Has no effect on α-adrenergic receptors. Also binds to 5HT-1B receptors with high affinity (Ki = 17 nM) in contrast to 5HT-1D receptors (Ki = 10.2 µM). Readily enters the central nervous system. Blocks phospholipase D-derived diacylglycerol (DAG) formation by inhibiting phosphatidate phosphohydrolase. Useful tool for discriminating between phospholipase D- or phospholipase C-mediated DAG production. An anti-hypertensive agent that is also used in the treatment of cardiac arrhythmias.
Biochem/physiol Actions
Cell permeable: no
Primary Target
β1 and β2 adrenergic receptors
β1 and β2 adrenergic receptors
Product does not compete with ATP.
Reversible: no
Target Ki: 17 nM for 5HT-1B receptors
Preparation Note
Following reconstitution, aliquot and freeze (-20°C).
Other Notes
Fujita, K., et al. 1996. FEBS Lett.395, 293.
Glennon, R.A., et al. 1996. Mol. Pharmacol.49, 198.
Thompson, N.T., et al. 1991. Trends Pharmacol. Sci.12, 404.
Hoffman, B.B., and Lefkowitz, R.J. 1990. in The Pharmacological Basis of Therapeutics (Gilman, A.G., et al., Eds.) p. 221, Pergamon Press, New York.
Glennon, R.A., et al. 1996. Mol. Pharmacol.49, 198.
Thompson, N.T., et al. 1991. Trends Pharmacol. Sci.12, 404.
Hoffman, B.B., and Lefkowitz, R.J. 1990. in The Pharmacological Basis of Therapeutics (Gilman, A.G., et al., Eds.) p. 221, Pergamon Press, New York.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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