Ajmalicine

SKU: orb1940249

Description

Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。(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.(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.

Key Properties

• CAS Number: 483-04-5
• MW: 352.43
• Purity: >98% (HPLC)
• 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
• Solubility: In Vitro: DMSO : 5.56 mg/mL (15.78 mM)

Bioactivity

• In Vivo:
  Ajmalicine blocking 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. Animal model: Male Wistar rats (300-350 g). Dosage: 0.5, 1, 2, and 4 mg/kg. Administration: IV, once. Result: Induced 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: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Raubasine | Delta-Yohimbine | Ajmalicin | Lamuran

Quick Database Links

Gene Symbol

Adrenergic Receptor