Home Neuronal Signaling Dopamine Receptor antagonist Rotundine For research use only.

Rotundine

Synonyms: L-tetrahydropalmatine, L-THP

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

Rotundine Chemical Structure

Rotundine Chemical Structure

CAS No. 483-14-7

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Rotundine Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Biological Activity

Description Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
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 Ki of 124 nM and 388 nM, respectively, while the IC50 values are 166 nM (D1) and 1.47 μM (D2), respectively. Rotundine exhibits a weak inhibitory activity against dopamine D3 with IC50 of 3.25 μM. Rotundine also potently inhibits 5-HT1A with IC50 of 374 nM and Ki of 340 nM. In addition to the antagonism of postsynaptic dopamine receptors, inhibition of presynaptic autoreceptors by Rotundine leads to increased dopamine release, which is probably attributed to lower affinity of Rotundine for D2 receptors. Along with dopamine receptors, Rotundine 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 Rotundine (10-25 mg/kg) significantly increases hot-plate latency of mice, indicating that Rotundine exerts remarkable analgesic activity, which is associated with β-endorphin neurons in the arcute nucleus and supraspinal D2 receptor. [3] Administration of Rotundine (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 Rotundine 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

Chemical Information & Solubility

Molecular Weight 355.43 Formula

C21H25NO4
CAS No. 483-14-7 SDF Download Rotundine SDF
Smiles COC1=C(C2=C(CC3C4=CC(=C(C=C4CCN3C2)OC)OC)C=C1)OC
Storage (From the date of receipt)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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