Ajmalicine

SKU: orb1685425

Description

Ajmalicine (Raubasine) is a potent α1-adrenoceptor antagonist with additional reversible, non-competitive inhibition of nicotinic receptors (IC50 = 72.3 µM). It is used in research as an anti-hypertensive and sedative agent, with applications in studying cardiovascular and neurological systems in vitro and in vivo.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 483-04-5
• MW: 352.43
• Purity: 96.90%
• Formula: C₂₁H₂₄N₂O₃
• SMILES: [H][C@@]12C[C@]3([H])C(=CO[C@@H](C)[C@@]3([H])CN1CCc1c2[nH]c2ccccc12)C(=O)OC
• Target: Adrenergic Receptor,Cholinesterase (ChE)
• Solubility: DMSO:2.5 mg/mL (7.09 mM)

Bioactivity

• In Vivo:
  Ajmalicine blocks the pressor action of electrical stimulation and is active against sympathetic stimulation. Ajmalicine (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline.
• In Vitro:
  Ajmalicine preferentially blocks α1-adrenoceptor than α2-adrenoceptor. Ajmalicine inhibits contractions in a concentration-dependent manner, IC50=72.3 ± 22.5 μM. Ajmalicine acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2.

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

α1-adrenoceptor, Δ-Yohimbine, Raubasine, Lamuran, Adrenergic Receptor, AdrenergicReceptor, Ajmalicin, Ajmalicine, Delta-Yohimbine

Compound Identifiers

PubChem CID

441975