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/ Phentolamine methanesulfonate salt

甲磺酸酚妥拉明 /Phentolamine methanesulfonate salt {[allProObj[0].p_purity_real_show]}

货号：A320047 同义名： Phentolamine methanesulfonate;Phentolamine mesylate

Phentolamine mesylate is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.

Phentolamine methanesulfonate salt 化学结构 CAS号：65-28-1
Phentolamine methanesulfonate salt 化学结构
CAS号：65-28-1
Phentolamine methanesulfonate salt 3D分子结构
CAS号：65-28-1
Phentolamine methanesulfonate salt 化学结构 CAS号：65-28-1
Phentolamine methanesulfonate salt 3D分子结构 CAS号：65-28-1
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Phentolamine methanesulfonate salt 纯度/质量文件 产品仅供科研

货号：A320047 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline hydrochloride ✔ 98%
Cisatracurium besylate ✔ 98%
Yohimbine HCI ✔ 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

 		+

β1-adrenoceptor, pIC50: 5.1

 		97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		97%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Doxazosin mesylate ✔ 98%
Tolazoline HCl ✔ 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Phentolamine methanesulfonate salt 生物活性

靶点

  • α-adrenergic receptor
描述 Phentolamine mesylate (OraVerse), a nonselective a-adrenergic blocking drug, is the first therapeutic agent marketed for the reversal of soft-tissue anaesthesia and the associated functional deficits resulting from an intraoral submucosal injection of a local anaesthetic containing a vasoconstrictor[3]. Phentolamine mesylate (PM) is widely used to reverse local anesthesia after dental procedures. PM substantially reduced the time to recovery of normal sensation and function after local anesthesia in routine dental treatment[4]. Phentolamine leads to an increase in FBM (fetal breathing movements) by preferentially antagonizing presynaptic alpha 2-adrenoreceptors over postsynaptic alpha 1-adrenoreceptors. This influence of phentolamine on FBM may be secondary to its effect on ECoG (electrocortical activity). Promotion of LV-ECoG by catecholamines is mediated via an alpha 1-independent mechanism[5]. Phentolamine mesylate, at dosages from 0.4 to 0.8 mg in adults and adolescents and at dosages from 0.2 to 0.4 mg in children aged 4 to 11 years, has been proven to be safe. Its ability to block a-adrenergic receptors on blood vessels induces vasodilation and enhances the redistribution of the local anesthetic away from the injection site[6].

Phentolamine methanesulfonate salt 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03240822 Urologic Injuries ... 展开 >> Genital Diseases, Male Amputation 收起 << Phase 1 Recruiting December 2025 United States, North Carolina ... 展开 >> Wake Forest School of Medicine Recruiting Winston-Salem, North Carolina, United States, 27104 Contact: Mary-Clare Day, RN BSN    336-713-1343    Mday@wakehealth.edu 收起 <<
NCT01422616 Ischemic Stroke ... 展开 >> High Blood Pressure 收起 << Phase 3 Recruiting February 2019 Australia, New South Wales ... 展开 >> Royal Prince Alfred Hospital Recruiting Sydney, New South Wales, Australia, 2050 Contact: Craig S Anderson, MD    +61 2 933 4500    canderson@georgeinstitute.org.au 收起 <<
NCT00226096 CVA (Cerebrovascular Accident)... 展开 >> Cerebral Hemorrhage Intracranial Hemorrhages 收起 << Not Applicable Completed - Australia, New South Wales ... 展开 >> Concord Hospital Concord, New South Wales, Australia, 2138 Gosford Hospital Gosford, New South Wales, Australia, 2250 St George Hospital Kogarah, New South Wales, Australia, 2217 John Hunter Hospital Newcastle, New South Wales, Australia, 2310 St Vincent's Hospital Sydney, New South Wales, Australia, 2010 Royal Prince Alfred Hospital Sydney, New South Wales, Australia, 2050 Westmead Hospital Westmead, New South Wales, Australia, 2145 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Australia, Victoria Royal Melbourne Hospital Melbourne, Victoria, Australia, 3050 St Vincent's Hospital Melbourne, Victoria, Australia, 3065 Box Hill Hospital Melbourne, Victoria, Australia, 3128 Alfred Hospital Melbourne, Victoria, Australia, 3181 Austin Health Melbourne, Victoria, Australia Monash Medical Centre Melbourne, Victoria, Australia Australia, Western Australia Sir Charles Gairdner Hospital Perth, Western Australia, Australia, 6009 China Regional Coordinating Centre: Peking University First Hospital Beijing, China, 100034 Hospitals in China, c/o The George Institute China Beijing, China Regional Coordinating Centre: Centre for Epidemiological Studies and Clinical Trials, Ruijin Hospital, Shanghai Institute of Hypertension, Shanghai Second Medical University Shanghai, China, 200025 New Zealand North Shore Hospital Auckland, New Zealand Christchurch Hospital Christchurch, New Zealand 收起 <<

Phentolamine methanesulfonate salt 参考文献

[1]Moore PA, Hersh EV, et al. Pharmacokinetics of lidocaine with epinephrine following local anesthesia reversal with phentolamine mesylate. Anesth Prog. 2008 Summer;55(2):40-8.

[2]Traish A, Gupta S, et al. Phentolamine mesylate relaxes penile corpus cavernosum tissue by adrenergic and non-adrenergic mechanisms. Int J Impot Res. 1998 Dec;10(4):215-23.

[3]Yagiela JA. What's new with phentolamine mesylate: a reversal agent for local anaesthesia?. SAAD Dig. 2011;27:3-7

[4]Daubländer M, Liebaug F, Niedeggen G, Theobald K, Kürzinger ML. Effectiveness and safety of phentolamine mesylate in routine dental care. J Am Dent Assoc. 2017;148(3):149-156

[5]Giussani DA, Moore PJ, Bennet L, Spencer JA, Hanson MA. Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero. J Physiol. 1995;486 (Pt 1)(Pt 1):249-255

[6]Hersh EV, Lindemeyer RG. Phentolamine mesylate for accelerating recovery from lip and tongue anesthesia. Dent Clin North Am. 2010;54(4):631-642

Phentolamine methanesulfonate salt 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.25mL

2.65mL

1.32mL

26.49mL

5.30mL

2.65mL

Phentolamine methanesulfonate salt 技术信息

CAS号65-28-1
分子式C18H23N3O4S
分子量 377.458
别名 Phentolamine methanesulfonate;Phentolamine mesylate;Phentolamine (mesylate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

H2O: 50 mg/mL(132.47 mM)
动物实验配方

Tags: Phentolamine | 65-28-1 | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Phentolamine methanesulfonate salt 纯度/质量文件 | Phentolamine methanesulfonate salt 亚型比较 | Phentolamine methanesulfonate salt 生物活性 | Phentolamine methanesulfonate salt 临床数据 | Phentolamine methanesulfonate salt 参考文献 | Phentolamine methanesulfonate salt 实验方案 | Phentolamine methanesulfonate salt 技术信息

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