(-)-Isocorypalmine  (Synonyms: Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine)

(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research^[1][2].

(-)-Isocorypalmine exhibits a D1 receptor expression-dependent agonistic effect on human dopamine D1 receptors. In HEK293 cells with high and moderate D1 receptor expression, the EC₅₀ values are 39 nM and 263 nM, respectively, while no agonistic effect is observed in cells with low D1 receptor expression. For the D5 receptor, (-)-Isocorypalmine has an EC₅₀ of 20 nM and a K_i of 9.5 nM; its K_i values for D2, D3, and D4 receptors are 41.8 nM, 37.3 nM, and 77.4 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(-)-Isocorypalmine (10 mg/kg; i.p.; single dose) produces a short-duration (~30 minutes) 55% reduction in novelty-induced spontaneous locomotor activity in male CD-1 mice^[1].
(-)-Isocorypalmine (1-10 mg/kg; i.p.; single dose) dose-dependently reduces acute cocaine-induced locomotor hyperactivity in male CD-1 mice, with complete inhibition at 10 mg/kg^[1].
(-)-Isocorypalmine (10 mg/kg; i.p.; once daily; 5 days) reduces acute cocaine-induced hyperlocomotion and blocks the development of repeated cocaine-induced locomotor sensitization in male CD-1 mice^[1].
(-)-Isocorypalmine (10 mg/kg; i.p.; once daily; 6 days) blocks the acquisition of cocaine-induced conditioned place preference in male CD-1 mice without inducing preference or aversion itself^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

341.40

C₂₀H₂₃NO₄

483-34-1

Solid

White to off-white

OC(C=C1[C@@]2([H])N3CC4=C(C=CC(OC)=C4OC)C2)=C(C=C1CC3)OC

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Xu W, et al. L-isocorypalmine reduces behavioral sensitization and rewarding effects of cocaine in mice by acting on dopamine receptors. Drug Alcohol Depend. 2013;133(2):693-703.

  [2]. Wang W, et al. Pharmacokinetics, tissue distribution, and excretion studies of l‐isocorypalmine using ultra high performance liquid chromatography with tandem mass spectrometry[J]. Journal of separation science, 2017, 40(5): 1040-1048.