CAS NO: | 43218-56-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
Storage | Store at -20°C |
M.Wt | 290.7 |
Cas No. | 43218-56-0 |
Formula | C12H18N2O4·HCl |
Solubility | insoluble in EtOH; ≥14.55 mg/mL in DMSO; ≥57.5 mg/mL in H2O |
Chemical Name | 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]-acetamide, monohydrochloride |
Canonical SMILES | OC(CNC(CN)=O)C1=C(OC)C=CC(OC)=C1.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Ki: 2, 6.9, and 1.7 μM for α1A, α1B, α1D, respectively
Midodrine is the prodrug of the α1-adrenergic receptor agonist, 1-(2’,5’-dimethoxyphenyl)-2-aminoethanol.
The α1-adrenergic receptor has some general functions similar with the α2-adrenergic receptor, but also has its own specific effects. α1-receptors primarily can mediate smooth muscle contraction and have other important functions as well.
In vitro: Midodrine was identified as a prodrug forming an active metabolite, desglymidodrine, which is an α1-receptor agonist exerting its actions through activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, leading to an increased vascular tone and elevation of blood pressure [1].
In vivo: A previous study was conducted to investigate the effect of intracerebroventricular injections of midodrine on the central nervous system of the rat. It was found that midodrine could decrease body temperature and increase locomotor activity, sedation in reserpinized rats as well as the cataleptic effect of haloperidol. Midodrine could also enhance amphetamine-stimulated locomotor activity and reduce the amphetamine and apomorphine sterotypy [1].
Clinical trial: The results of a previous pilot study indicated that midodrine combination with tolvaptan could better control ascites without any hepatic or renal dysfunction. Such combination therapy controled ascites rapidly as compared to midodrine or tolvaptan alone [2].
References:
[1] Kleinrok Z, Jagieo-Wójtowicz E, Oktaba-Polkowska A. Central action of intraventricularly-injected midodrine in rats. Arch Int Pharmacodyn Ther. 1980 Oct;247(2):217-33.
[2] Rai N, Singh B, Singh A, Vijayvergiya R, Sharma N, Bhalla A, Singh V. Midodrine and tolvaptan in patients with cirrhosis and refractory or recurrent ascites: a randomised pilot study. Liver Int. 2017 Mar;37(3):406-414.