U101
5-Methylurapidil
solid
别名:
5-Methyl-6[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil
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关于此项目
经验公式（希尔记法）:
C21H31N5O3
化学文摘社编号:
分子量:
401.50
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C21H31N5O3.ClH/c1-16-19(23(2)21(28)24(3)20(16)27)22-10-7-11-25-12-14-26(15-13-25)17-8-5-6-9-18(17)29-4;/h5-6,8-9,22H,7,10-15H2,1-4H3;1H
SMILES string
Cl[H].COc1ccccc1N2CCN(CCCNC3=C(C)C(=O)N(C)C(=O)N3C)CC2
InChI key
WAZDYFHTLYHMKO-UHFFFAOYSA-N
form
solid
color
white
solubility
H2O: 0.4 mg/mL, 0.1 M HCl: 3.8 mg/mL
Quality Level
Gene Information
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
Application
5-Methylurapidil has been used for competitive binding in radioligand binding assays.
Biochem/physiol Actions
Selective α1A-adrenoceptor antagonist; antihypertensive.
Features and Benefits
This compound is featured on the α1-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Preparation Note
5-Methylurapidil is soluble in water at 0.4 mg/ml and is also soluble in 0.1 M HCl at 3.8 mg/ml.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
M Endoh et al.
Naunyn-Schmiedeberg's archives of pharmacology, 345(5), 578-585 (1992-05-01)
In order to elucidate the contribution of alpha 1A subtype to the positive inotropic effect mediated by myocardial alpha 1 adrenoceptors, the influence of the alpha 1A selective antagonists WB 4101 and 5-methylurapidil on the alpha 1-mediated positive inotropic effect
G Gross et al.
European journal of pharmacology, 169(2-3), 325-328 (1989-10-10)
Radioligand binding studies suggest that alpha 1-adrenoceptor recognition sites are heterogeneous. Several adrenergic agents discriminate between two adrenoceptor binding sites designated alpha 1A and alpha 1B. In the present study we demonstrate for the first time that these two subtypes
Claudia Roberta de Andrade et al.
European journal of pharmacology, 543(1-3), 83-91 (2006-07-11)
Hyperhomocysteinemia is a known risk factor for cardiovascular diseases, but the underlying mechanisms of this pathology are complex. We aimed to evaluate the effect of hyperhomocysteinemia in vasorelaxations induced by alpha(1D)-adrenoceptor agonists. Vascular reactivity of rat carotid artery to the
G Gross et al.
European journal of pharmacology, 151(2), 333-335 (1988-07-07)
The affinity of 5-methyl-urapidil for alpha 1-adrenoceptors was determined from the inhibition of [3H]prazosin binding on membrane of different rat tissues. In hippocampus, vas deferens and heart 5-methyl-urapidil displaced [3H]prazosin in a biphasic manner with mean pKI values between 9.1
D W Gil et al.
British journal of pharmacology, 153(4), 769-774 (2007-08-19)
The most common preclinical models of neuropathic pain involve surgical ligation of sensory nerves, which is especially difficult in mice. Transient models of chemically sensitized allodynia are potentially useful for rapidly characterizing the analgesic profile of compounds and conducting mechanistic
商品
Review alpha 1 adrenoceptors as well as their agonists, antagonists, and tissue expression patterns. We suggest several modulators and alternatives for working with a-1 adrenoreceptors.
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