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Phentolamine mesylate

CAS号

65-28-1

分子式

C17H19N3O·CH4O3S

主要靶点

Adrenergic Receptor

仅限科研使用

Cat No : CM02562

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Synonyms

adrenergic|AdrenergicReceptor|Adrenergic Receptor|blood|Beta Receptor|dysfunction|heart|hypertension|erectile|failure|resistance|peripheral|Phentolamine mesilate|Phentolamine mesylate|Phentolamine Mesylate|Phentolamine methanesulfonate|Phentolamine|pheochromocytoma|Inhibitor|inhibit|甲磺酸酚妥拉明|vessels|α-adrenergic receptor|vascular

验证数据展示

  • CAS No.: 65-28-1

    Phentolamine mesylate
    CAS#: 65-28-1

产品信息

CAS号 65-28-1
分子式 C17H19N3O·CH4O3S
主要靶点 Adrenergic Receptor
主要通路 神经科学|G 蛋白偶联受体
分子量 377.46
纯度 99.9%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 adrenergic|AdrenergicReceptor|Adrenergic Receptor|blood|Beta Receptor|dysfunction|heart|hypertension|erectile|failure|resistance|peripheral|Phentolamine mesilate|Phentolamine mesylate|Phentolamine Mesylate|Phentolamine methanesulfonate|Phentolamine|pheochromocytoma|Inhibitor|inhibit|甲磺酸酚妥拉明|vessels|α-adrenergic receptor|vascular

靶点活性

α-adrenoceptor:5 - 30 nM

体内活性

Phentolamine是一种可逆的竞争性α-肾上腺素受体拮抗剂，对α1和α2受体具有相似的亲和力。Phentolamine mesylate 通过降低外周血管阻力，导致血管舒张从而降低血压。[4] Phentolamine mesylate （30和100纳摩尔浓度）对兔子阴茎海绵体电场刺激引起的舒张作用有剂量依赖性的增强作用。酚妥拉明能独立于α-肾上腺素受体阻断放松兔子阴茎海绵体。Phentolamine mesylate 通过激活NO合成酶放松兔子阴茎海绵体的非肾上腺素非胆碱能神经元，这种放松作用与α-肾上腺素受体阻断无关。[5]

体外活性

Phentolamine mesylate在海绵体膜中与选择性α1受体拮抗剂[125I]HEAT和[3H]prazosin以及α2受体拮抗剂[3H]rauwolscine和[3H]RX 821002竞争结合，展示出相对高的亲和力。在以肾上腺素激动剂苯肾上腺素、去甲肾上腺素、氧美唑林和UK 14,304以及非肾上腺素收缩剂Endothelin和KCl预收缩的勃起组织条带中，Phentolamine mesylate引起浓度依赖性的松弛。Phentolamine mesylate通过直接拮抗α1和α2肾上腺素受体以及通过非肾上腺素、内皮介导机制（暗示一氧化氮合酶激活）的间接功能拮抗诱发海绵体勃起组织的松弛。[1] Phentolamine作为一种α-肾上腺素拮抗剂，阻断与用于牙科麻醉配方中的肾上腺素相关的血管收缩，从而增强了从注射部位的局部麻醉剂的系统吸收。[2]

溶解度

H2O:37.8 mg/mL (100.14 mM);DMSO:60 mg/mL (158.96 mM)

参考文献

1.Traish A, et al. Int J Impot Res,1998, 10(4), 215-223.
2.Moore PA, et al. Anesth Prog,2008, 55(2), 40-48.
3.Holt A, et al. J Pharm Pharmacol,1995, 47(10), 837-845.
4.Vemulapalli S, et al. Fundam Clin Pharmacol,2001, 15(1), 1-7.

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