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Rotundine Dopamine Receptor antagonist

Name: Rotundine
Brand: Selleck Chemicals
SKU: S2437
Availability: InStock
Rating: 5 (1 reviews)

Catalog No.S2437 Purity:99.99%

Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.

Chemical Structure

Molecular Weight: 355.43

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Signaling Pathway

Dopamine Receptor Signaling Pathway

Mechanism of Action

Targets

D1 receptor ^[1]	5-HT1A ^[1]	D2 receptor ^[1]	D3 receptor ^[1]
166 nM	347 nM	1.47 μM	3.25 μM

In vitro
In vitro	Rotundine displays a higher affinity to dopamine D1 than D2 receptor with K_i of 124 nM and 388 nM, respectively, while the IC50 values are 166 nM (D1) and 1.47 μM (D2), respectively. This compound exhibits a weak inhibitory activity against dopamine D3 with IC50 of 3.25 μM. It also potently inhibits 5-HT1A with IC50 of 374 nM and K_i of 340 nM. In addition to the antagonism of postsynaptic dopamine receptors, inhibition of presynaptic autoreceptors by this chemical leads to increased dopamine release, which is probably attributed to lower affinity of this compound for D2 receptors. Along with dopamine receptors, it can interact with a number of other receptor types, including α-1 adrenergic receptors, at which it functions as an antagonist, and γ-aminobutyric acid receptors, at which it facilitates γ-aminobutyric acid binding through positive allosteric effects. ^[1]

In Vivo
In vivo	Rotundine treatment does not affect the locomotor activity at the doses of 6.25 mg/kg, 12.5 mg/kg, or 18.75 mg/kg, but significantly antagonizes the hyperactivity induced by oxy-codone (5 mg/kg). ^[2] Oral administration of this compound (10-25 mg/kg) significantly increases hot-plate latency of mice, indicating that this compound exerts remarkable analgesic activity, which is associated with β-endorphin neurons in the arcute nucleus and supraspinal D2 receptor. ^[3] Administration of this chemical (1-10 mg/kg) dose-dependently increases, while 20 mg/kg decreases the rate of cocaine self-administration under fixed-ratio (FR) reinforcement, due to a postsynaptic, rather than presynaptic, DA receptor blockade mechanism. In contrast to the effects on cocaine's actions, only the 10 mg/kg dose of this compound but not 1 mg/kg or 3 mg/kg produces inhibitory effect on sucrose self-administration and locomotion. ^[4] LD50: Mice 1160mg/kg (i.g.) ^[5]
Animal Research	Animal Models	Female ICR mice subjected to hot plate latency assay
	Dosages	25 mg/kg
	Administration	Oral administration

References

https://pubmed.ncbi.nlm.nih.gov/22300097/
https://pubmed.ncbi.nlm.nih.gov/15842769/
https://pubmed.ncbi.nlm.nih.gov/15635188/

https://pubmed.ncbi.nlm.nih.gov/17888459/
http://www.ingentaconnect.com/content/ben/lddd/2011/00000008/00000005/art00009

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Chemical Information

Molecular Weight	355.43	Formula	C₂₁H₂₅NO₄
CAS No.	483-14-7	SDF	Download SDF
Synonyms	L-tetrahydropalmatine, L-THP
Smiles	COC1=C(C2=C(CC3C4=CC(=C(C=C4CCN3C2)OC)OC)C=C1)OC

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 8 mg/mL ( (22.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.850mg/ml (10.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.52mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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