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Rotundine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rotundine图片
CAS NO:483-14-7
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)355.43
FormulaC21H25NO4
CAS No.483-14-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 8 mg/mL (22.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: (5S)-3,8-dimethoxy-13-methyl-5,6,11,12-tetrahydro-5,11-epiminodibenzo[a,e][8]annulene-2,9-diol

InChi Key: JLYWCHLTLCGOMW-LOACHALJSA-N

InChi Code: InChI=1S/C19H21NO4/c1-20-14-4-10-6-16(21)19(24-3)9-13(10)15(20)5-11-7-18(23-2)17(22)8-12(11)14/h6-9,14-15,21-22H,4-5H2,1-3H3/t14?,15-/m0/s1

SMILES Code: OC1=C(OC)C=C2C(CC3C4=CC(O)=C(OC)C=C4C[C@]2([H])N3C)=C1

Synonyms

(-)-Tetrahydropalmatine; L-Tetrahydropalmatine; Rotundine

实验参考方法
In Vitro

In vitro activity: 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.

In VivoRotundine 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 oxycodone (5 mg/kg). 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. 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.
Animal modelFemale ICR mice subjected to hot plate latency assay
Formulation & DosageDissolved in saline; 25 mg/kg; Oral gavage
References

Future Med Chem. 2012 Feb;4(2):177-86; Acta Pharmacol Sin. 2005 May;26(5):533-8.