Isoprenaline hydrochloride

SKU: orb1224862

Description

Isoprenaline Hydrochloride is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.(In Vitro):Isoprenaline (Isoproterenol) hydrochloride (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells.Isoprenaline inhibits insulin-stimulated glucose transport activity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approximately 2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of > 50%, which directly correlated with the observed inhibition of transport activity.Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO).Isoprenaline increases the transcriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gs alpha remains unchanged.Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift of approximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+ current.Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells.(In Vivo):Isoprenaline (Isoproterenol) hydrochloride (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs.

Key Properties

• CAS Number: 51-30-9
• MW: 247.72
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₈ClNO₃
• SMILES: OC(CNC(C)C)C1=CC=C(O)C(O)=C1.[H]Cl
• Target: Adrenergic Receptor
• Solubility: Water: 50 mg/mL (201.84 mM); DMSO: 50 mg/mL (201.84 mM)

Bioactivity

• In Vivo:
  Isoprenaline (Isoproterenol) hydrochloride (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs. Animal model: Dogs. Dosage: 0.27-0. 64 μg/kg. Administration: oral. Result: Excreted largely unchanged in urine, only one-third of the radioactivity in urine was in the form of the O-methyl metabolite. Showed plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine. Showed heart rate returned to base-line values when high plasma concentrations.
• In Vitro:
  Isoprenaline (Isoproterenol) hydrochloride (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells. Isoprenaline inhibits insulin-stimulated glucose transport activity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approximately 2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of > 50%, which directly correlated with the observed inhibition of transport activity. Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO). Isoprenaline increases the transcriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gs alpha remains unchanged. Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift of approximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+ current. Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Isoprenaline | NSC 37745 | NSC 89747

Quick Database Links

Gene Symbol

Adrenergic Receptor