HEAT hydrochloride
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively.
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- CAS. Nr.: 30007-39-7
- Formel: C19H22ClNO2
- Molecular Weight:331.84
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Biologische Aktivität
Beschreibung
In Vitro
BE2254 inhibits (-)-noradrenaline-mediated increases in gluconeogenesis with K,sub>B of 0.74 nM[2].
The alpha-1 selective antagonist [125I]BE2254 is used to specifically label a single class of binding sites with a dissociation constant of 131.0 pM and a maximal binding capacity of 17.6 fmol/mg of protein. Catecholamines compete for [125I]BE2254 binding stereospecifically and with the characteristic alpha adrenergic potency series of (-)-epinephrine greater than (-)-norepinephrine much greater than (-)-isoproterenol. The alpha-1 selective antagonist prazosin (Kd=2.4 nM) is much more potent in competing for [125I]BE2254 binding than is the alpha-2 selective antagonist yohimbine (Kd=2900 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 30007-39-7
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Molecular Weight 331.84
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Formel C19H22ClNO2
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SMILES
O=C1C(CNCCC2=CC=C(O)C=C2)CCC3=C1C=CC=C3.Cl
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Synonyms
BE2254 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Chiu G, et al. Design and synthesis of an alpha1a-adrenergic receptor subtype-selective antagonist from BE2254. Chem Biol Drug Des. 2006;67(6):437-439. [Content Brief]
[2]. McPherson GA, et al. A study of alpha 1-adrenoceptors in rat renal cortex: comparison of [3H]-prazosin binding with the alpha 1-adrenoceptor modulating gluconeogenesis under physiological conditions. Br J Pharmacol. 1982;77(1):177-184. [Content Brief]
[3]. Tsujimoto G, et al. Alpha adrenergic receptors in the rabbit bladder base smooth muscle: alpha-1 adrenergic receptors mediate contractile responses. J Pharmacol Exp Ther. 1986;236(2):384-389. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
HEAT hydrochloride Related Classifications
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