Phenoxybenzamine HCl

SKU: orb1309567

Description

Phenoxybenzamine hydrochloride is an irreversible, non-selective alpha-adrenergic antagonist used in research for its vasodilatory effects. It is applied in studies of hypertension, pheochromocytoma, and autonomic pharmacology, utilizing both in vitro receptor binding assays and in vivo models to investigate peripheral resistance and reflex tachycardia.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 63-92-3
• MW: 340.29
• Purity: >98%
• Formula: C₁₈H₂₂ClNO · HCl
• SMILES: Cl.CC(COc1ccccc1)N(CCCl)Cc1ccccc1
• Target: GPCR
• Solubility: Soluble in DMSO (up to 50 mg/ml), or in Water (up to 15 mg/ml).

Bioactivity

• In Vivo:
  Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice and the cell density in Phenoxybenzamine hydrochloride-U87 mg xenografts decreases significantly. Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS and foot fault scoring.
• In Vitro:
  The IC50 (100 nM) derived from the blockade of [3H]yohimbine binding by Phenoxybenzamine hydrochloride is significantly less than the IC50 (550 nM) for the corresponding reversal by Phenoxybenzamine hydrochloride of the effects of norepinephrine on cyclic AMP accumulation. Phenoxybenzamine hydrochloride (50 nM) in conbination with Phenoxybenzamine hydrochloridetolamine (1000 nM) enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with pretreatment with Phenoxybenzamine hydrochloride (50 nM) alone in endothelium-intact aortae. Combined treatment with either dexmedetomidine (300 or 1000 nM) and Phenoxybenzamine hydrochloride (50 nM) or Phenoxybenzamine hydrochloridetolamine (1000 nM) and Phenoxybenzamine hydrochloride (50 nM) enhance Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with Phenoxybenzamine hydrochloride alone (50 nM). In addition, combined treatment with Phenoxybenzamine hydrochloridetolamine and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride combined treatment. Combined treatment with high concentrations of dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with combined treatment with low concentrations of dexmedetomidine (300 nM) and Phenoxybenzamine hydrochloride.
• Cell Research:
  Phenoxybenzamine hydrochloride is dissolved in DMSO. After cytometry, 1×3 cells are implanted in a 96-well plate in 100 μL DMEM supplemented with 10 % FBS. Ten microliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37°C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The mean fluorescence value is counted, and the cell number is determined using the standard curve.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AdrenergicReceptor, Adrenergic Receptor, CAM, antitumor, Beta Receptor, glioma, hypertension, Inhibitor, NSC 37448, inhibit, NCI-c01661, neuroprotective, NSC37448, NSC-37448, pheochromocytoma, Phenoxybenzamine, Phenoxybenzamine HCl, Phenoxybenzamine hydrochloride, Phenoxybenzamine Hydrochloride, α-adrenergic receptor

Compound Identifiers

PubChem CID

5284441