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tetrahydropalmatine
- Development stage
- Phase 2
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Tetrahydropalmatine is an isoquinoline alkaloid found primarily in plants of the Corydalis and Stephania genera. It is widely used in China as a sedative and analgesic agent. Tetrahydropalmatine acts mainly as a dopamine receptor antagonist and also blocks other monoamine receptors. It has additional pharmacological actions including blockade of voltage-activated L-type calcium channels and activation of potassium channels. The compound exhibits muscle relaxant properties and has been investigated for its potential use in treating schizophrenia, drug addiction (notably cocaine use disorder), anxiety, insomnia, heart disease, liver damage, neuropathic pain, inflammatory diseases, dysmenorrhea, cancer-related symptoms, and brain edema[1][2][3][5][6][8]. Its mechanism involves modulation of dopaminergic neurotransmission as well as possible effects on GABAA receptor benzodiazepine sites[5][6]. Tetrahydropalmatine is considered non-addictive with a favorable safety profile at therapeutic doses.
- Brand names
- RotundineRotundine HCl
- Other names
- THPl-THPdl-THPlevo-tetrahydropalmatine
02
Targets
HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)BZD site (GABA-A receptor benzodiazepine site)TAAR1 (Trace amine-associated receptor 1)KCNK1 (Potassium channel subfamily K member 1)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)
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