Naftopidil

SKU: orb1310376

Description

Naftopidil (Flivas, KT-611) is a selective α1-adrenergic receptor antagonist used as an antihypertensive agent. It is employed in pharmacological research to study receptor function and has been utilized in both in vitro binding assays and in vivo models of hypertension and benign prostatic hyperplasia.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57149-07-2
• MW: 392.49
• Purity: 99.97% (May vary between batches)
• Formula: C₂₄H₂₈N₂O₃
• SMILES: O(CC(CN1CCN(CC1)C2=C(OC)C=CC=C2)O)C=3C4=C(C=CC3)C=CC=C4
• Target: Adrenergic Receptor
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.1 mM);DMSO:75 mg/mL (191.09 mM)

Bioactivity

• Target IC50:
  α1D-adrenoceptor:1.2 nM(Ki)|α1A-adrenoceptor:3.7 nM(Ki)|α1B-adrenoceptor:20 nM(Ki)
• In Vivo:
  Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats.
• In Vitro:
  Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil induces p21(cip1) but not p27(kip1) in PC-3 cells. Naftopidil induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Naftopidil-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. Naftopidil, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM Naftopidil. Naftopidil also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. Naftopidil (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. Naftopidil inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. Naftopidil binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Naftopidil, inhibit, KT611, KT-611, KT 611, Inhibitor, hyperplasia, Beta Receptor, BM 15275, BM15275, BM-15275, canine, Adrenergic Receptor, AdrenergicReceptor, prostatic, prostate, pressure, α1A-adrenergic receptor, α1D-adrenergic receptor, α1B-adrenergic receptor

Compound Identifiers

PubChem CID

4418