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Carazolol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Carazolol图片
CAS NO:57775-29-8
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
250mg电议

产品介绍
Carazolol 是一种高效的 β1/β2 肾上腺素受体拮抗剂,用于高血压研究。
Cas No.57775-29-8
别名卡拉洛尔; (±)-Carazolol; DL-Carazolol; Suacron
化学名1-(9H-carbazol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol
Canonical SMILESOC(CNC(C)C)COC1=C(C(C=CC=C2)=C2N3)C3=CC=C1
分子式C18H22N2O2
分子量298.4
溶解度≥ 14.8mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Carazolol is a high-affinity, lipophilic, and non-selective ligand of the β-adrenergic receptors [1,2].

β-adrenergic receptors have been involved in mediating the physiological responses of the catecholamines, epinephrine and norepinephrine and modulating a myriad of physiological functions, such as relaxation of smooth muscle, chronotropic and inotropic cardiac responses, and lipolysis in adipose tissue. The β-adrenergic receptors exist in nearly all mammalian tissues. Until now, three β-adrenergic receptors have been identified, β1-, β2- and β3-adrenergic receptors [3].

In CHO cells expressing the human β3-adrenoceptor, the Ki value of carazolol was 2.0 ± 0.2 and the IC50 was 11.3 ± 1.2 nM. Carazolol exhibited an ECs0 of 25 nM and behaved as a full agonist (intrinsic activity = 0.97) towards the murine β3-adrenoceptor. In murine 3T3-F442A-derived adipocytes express the β3-adrenoceptor, carazolol stimulated lipolysis [1]. Carazolol bound to cortical β-receptors with a Kd value of 0.15 nM. Carazolol showed equal displacements constants when binding with calf cerebral cortex (which contained mainly β1 receptors) and calf cerebellum (which contained mainly β2 receptors), indicating that carazolol bound with equal affinity to β1 and β2 receptors [2].

References:
[1] Méjean A, Guillaume J L, Strosberg A D.  Carazolol: a potent, selective β3-adrenoceptor agonist[J]. European Journal of Pharmacology: Molecular Pharmacology, 1995, 291(3): 359-366.
[2] Innis R B, Corrêa F M A, Snyder S H.  Carazolol, an extremely potent β-adrenergic blocker: Binding to β-receptors in brain membranes [J]. Life sciences, 1979, 24(24): 2255-2264.
[3] Pellegrino S M, Lee N H, Fraser C M.  β-Adrenergic receptors[J]. Biomembranes: A Multi-Volume Treatise, 1996, 2: 245-279.