1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. Rotundine

Rotundine  (Synonyms: (-)-Tetrahydropalmatine; L-Tetrahydropalmatine)

Cat. No.: HY-N0096 Purity: 99.87%
COA Handling Instructions

Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.

For research use only. We do not sell to patients.

Rotundine Chemical Structure

Rotundine Chemical Structure

CAS No. : 483-14-7

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.

IC50 & Target

D1 Receptor

166 nM (IC50)

D2 Receptor

1400 nM (IC50)

D3 Receptor

3300 nM (IC50)

5-HT1A Receptor

370 nM (IC50)

In Vivo

It is reported that Rotundine (l-THP) possesses a blocking effect on dopamine D1 and D2 receptors and can inhibit physical dependence in morphine dependent mice and significantly reduce the development of the conditional place preference induced by morphine in mice. On day 1 and 7, there is no difference in locomotor counts between the Rotundine groups (6.25, 12.5, and 18.75 mg/kg) and saline group [F(3, 37)=1.360, P>0.05, F(3, 37)=0.348, P>0.05, respectively]. Locomotor counts are greatly increased in the oxycodone group compare with the saline group. Rotundine at doses of 6.25, 12.5, and 18.75 mg/kg antagonizes hyperactivity induced by oxycodone [F(4, 60)=15.76, P<0.01]. Rotundine (6.25, 12.5 mg/kg) does not affect the magnitude of sensitization, but there is a marked difference between oxycodone+oxycodone group and Rotundine (18.75 mg/kg)+oxycodone+oxycodone group, indicating that Rotundine (18.75 mg/kg) greatly inhibits the development of oxycodone sensitization [F(4, 62)=8.766, P<0.01][2].

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

Molecular Weight

355.43

Formula

C21H25NO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C2C(CN3CCC4=CC(OC)=C(OC)C=C4[C@]3([H])C2)=C1OC

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (281.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8135 mL 14.0675 mL 28.1349 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[2]

Kunming mice, initially weighing 18 to 22 g are used in this study. Four groups of mice are given Rotundine (l-THP) (6.25, 12.5, and 18.75 mg/kg) or saline, respectively, once per day for 7 consecutive days, followed by a 5 d withdrawal period. On d 13, all animals are challenged with saline. On day 1, 7, and 13, after 40-min treatment with Rotundine or saline, the mice are put into the test boxes and locomotor activity is monitored for 60 min[2].

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

References

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8135 mL 14.0675 mL 28.1349 mL 70.3373 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 mL 14.0675 mL
10 mM 0.2813 mL 1.4067 mL 2.8135 mL 7.0337 mL
15 mM 0.1876 mL 0.9378 mL 1.8757 mL 4.6892 mL
20 mM 0.1407 mL 0.7034 mL 1.4067 mL 3.5169 mL
25 mM 0.1125 mL 0.5627 mL 1.1254 mL 2.8135 mL
30 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3446 mL
40 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
50 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
60 mM 0.0469 mL 0.2345 mL 0.4689 mL 1.1723 mL
80 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
100 mM 0.0281 mL 0.1407 mL 0.2813 mL 0.7034 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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