Tetrahydropalmatine - CAS 2934-97-6
Catalog number: B0084-474737
Category: Inhibitor
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Molecular Formula:
C21H25NO4
Molecular Weight:
355.434
COA:
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Targets:
Dopamine Receptor
Description:
Tetrahydropalmatine is isolated from the Chinese herb corydalis and acts as a striatal dopamine D2 receptor antagonist in rats. Tetrahydropalmatine exhibits analgesic effect, and may be a potential treatment of heart disease, liver damage and certain drug addiction.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474737 5 g $229 In stock
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Brife Description:
dopamine D2 receptor antagonist
Purity:
≥ 98%
Appearance:
White Crystalline Powder
Synonyms:
Rotundine; Tetrahydropalmatin; 2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline
MSDS:
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Application:
analgesic; potential treatment of heart disease, liver damage and certain drug addiction
Shelf Life:
2 years
Boiling Point:
482.9±45.0 °C | Condition: Press: 760 Torr
Melting Point:
145 °C
Density:
1.23 g/cm3
InChIKey:
AEQDJSLRWYMAQI-UHFFFAOYSA-N
InChI:
InChI=1S/C21H25NO4/c1-23-18-6-5-13-9-17-15-11-20(25-3)19(24-2)10-14(15)7-8-22(17)12-16(13)21(18)26-4/h5-6,10-11,17H,7-9,12H2,1-4H3
Canonical SMILES:
COC1=C(C2=C(CC3C4=CC(=C(C=C4CCN3C2)OC)OC)C=C1)OC
1.Levo-tetrahydropalmatine, a natural, mixed dopamine receptor antagonist, inhibits methamphetamine self-administration and methamphetamine-induced reinstatement.
Gong X1, Yue K1, Ma B1, Xing J1, Gan Y2, Wang D2, Jin G3, Li C4. Pharmacol Biochem Behav. 2016 May;144:67-72. doi: 10.1016/j.pbb.2016.01.010. Epub 2016 Jan 21.
Despite the high prevalence of methamphetamine (METH) use, no FDA-approved pharmacological treatment is currently available for individuals with a METH addiction. Levo-tetrahydropalmatine (l-THP) is an alkaloid substance derived from corydalis and stephania that has been used in traditional Asian medicine for its analgesic, sedative and hypnotic properties. Previous pharmacological studies of l-THP indicated that it not only binds to D1 and D2 receptors but also has a low affinity for D3 receptors and may function as an antagonist. The unique pharmacological profile of l-THP suggests that it may have potential therapeutic effects on drug addiction; however, the effects of l-THP in individuals with METH addictions are largely unknown. In this study, we investigated the effects of l-THP on METH self-administration and METH-induced reinstatement. In our experiments, l-THP (1.25, 2.50 and 5.00mg/kg, i.p.) decreased METH self-administration under the fixed-ratio 1 schedule.
2.Tetrahydropalmatine attenuates irradiation induced lung injuries in rats.
Yu J1, Che J1, Liu L1, Yang F1, Zhu X2, Cao B3. Life Sci. 2016 Apr 6. pii: S0024-3205(16)30202-8. doi: 10.1016/j.lfs.2016.03.056. [Epub ahead of print]
AIMS: The lung is a major organ targeted by irradiation (R) in cancer radiotherapy of the thoracic region. Irradiation induced lung injury (RILI) is a common major obstacle in thoracic cancer radiotherapy. Tetrahydropalmatine (THP) has been shown to have a protective effect against oxidative stress. This study was designed to investigate the potential radioprotective effect of THP against RILI and to elucidate the underlying mechanisms.
3.Combination of Levo-Tetrahydropalmatine and Low Dose Naltrexone: A Promising Treatment for Prevention of Cocaine Relapse.
Sushchyk S1, Xi ZX1, Wang JB2. J Pharmacol Exp Ther. 2016 May;357(2):248-57. doi: 10.1124/jpet.115.229542. Epub 2016 Feb 22.
Relapse to drug use is often cited as the major obstacle in overcoming a drug addiction. Whereas relapse can occur for a myriad of reasons, it is well established that complex neuroadaptations that occur over the course of addiction are major factors. Cocaine, as a potent dopamine transporter blocker, specifically induces alterations in the dopaminergic as well as other monoaminergic neurotransmissions, which lead to cocaine abuse and dependence. Evidence also suggests that adaptations in the endogenous opioids play important roles in pathophysiology of cocaine addiction. Following this evidence, we investigated a combination medication, levo-tetrahydropalmatine (l-THP) and low dose naltrexone (LDN), targeting primarily dopaminergic and endogenous opioid systems as a cocaine-relapse-prevention treatment. In the present study Wistar rats were used to assess the effects ofl-THP and LDN on cocaine self-administration, drug-seeking behavior during cocaine reinstatement, spontaneous locomotion, and effects on the endogenous opioid system.
4.L-Tetrahydropalmatine alleviates mechanical hyperalgesia in models of chronic inflammatory and neuropathic pain in mice.
Zhou HH1, Wu DL, Gao LY, Fang Y, Ge WH. Neuroreport. 2016 May 4;27(7):476-80. doi: 10.1097/WNR.0000000000000560.
Chronic pain is categorized as inflammatory and neuropathic, and there are common mechanisms underlying the generation of each pain state. Such pain is difficult to treat and the treatment at present is inadequate. Corydalis yanhusuo is a traditional Chinese medicine with demonstrated analgesic efficacy in humans. The potential antihyperalgesic effect of its active component is L-tetrahydropalmatine (L-THP). L-THP has been used for the treatment of headache and other mild pain. However, little is known about its analgesic effect on chronic pain and its mechanism. Here, we report that L-THP exerts remarkable antihyperalgesic effects on neuropathic and inflammatory pain in animal models. Neuropathic hypersensitivity was induced by segmental spinal nerve ligation and inflammatory hypersensitivity was induced by an intraplantar injection of complete Freund's adjuvant. To determine the receptor mechanism underlying the antihyperalgesic actions of L-THP, we used SCH23390, an antagonist of a dopamine D1 receptor, in an attempt to block the antihyperalgesic effects of L-THP.
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CAS 2934-97-6 Tetrahydropalmatine

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