HEAT hydrochloride  (Synonyms: BE2254 hydrochloride)

HEAT (BE2254) hydrochloride is a selective _{alpha 1 adrenergic receptor} antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pK_is of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively^[1][2].

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 (K_d=2.4 nM) is much more potent in competing for [¹²⁵I]BE2254 binding than is the alpha-2 selective antagonist yohimbine (K_d=2900 nM)^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

331.84

C₁₉H₂₂ClNO₂

30007-39-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]