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Naftopidil (Flivas) is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM. Naftopidil (Flivas) is an antihypertensive agent. Naftopidil (Flivas) binds specifically to alpha 1-adrenoceptors. The Ki values are 58.3 nM for naftopidil, 0.43 nM for prazosin, and 197 nM for urapidil. The affinities of naftopidil to alpha 2- and beta-adrenoceptor sites are very low (> 6,000 and > 2,500 nM). Naftopidil relaxes aortic strips precontracted with norepinephrine concentration-dependently, and naftopidil (Flivas) shifts the concentration-response curve of norepinephrine in a parallel manner to the right. The pA2 values are 7.10 for naftopidil, 8.85 for prazosin, and 6.25 for urapidil.
| Molecular Weight | 392.49 |
| Formula | C24H28N2O3 |
| CAS Number | 57149-07-2 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Adrenergic Receptor Products |
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| Tamsulosin hydrochloride
Tamsulosin is a new, highly selective α1A-adrenoceptor antagonist. |
| Mirabegron
Mirabegron (YM178) is a potent and selective β(3)-adrenoceptor agonist with EC50 of 22.4 nM. |
| Detomidine hydrochloride
Detomidine hydrochloride is a nonnarcotic, synthetic alpha-2 adrenoreceptor agonist. |
| (R)-(+)-Atenolol
(R)-(+)-Atenolol binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. |
| Reboxetine mesylate
Reboxetine mesylate is a potent and selective inhibitor of noradrenalin uptake (Ki values are 1.1, 129 and > 10000 nM for rat NET, SERT and DAT respectively). |
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