Dopaminergic unique affinity of tetrahydroberberine and l-tetrahydroberberine-d-camphor sulfonate.
l-Tetrahydroberberine-d-camphor sulfonate (THB-CS) possessed an inhibitory effect on apomorphine-induced chewing movement in a similar manner to that of tetrahydroberberine (THB). Both compounds enhanced barbiturate-induced hypnosis. They did not have an anticonvulsant effect on convulsive seizures induced by bicuculline, pentetrazole or strychnine. THB and THB-CS blocked dopamine-stimulated adenylate cyclase activity. These compounds showed almost equipotent affinities to dopamine D1 (3H-SCH-23390) and D2 (3H-spiperone) receptors but did not have significant affinity to mu-opioid, muscarinic and alpha 2-adrenergic receptors, and benzodiazepine binding sites. Furthermore, both compounds did not elicit cataleptogenic behavior, even at very high doses. These data suggest that THB and THB-CS have a central depressant effect through both D1 and D2 dopaminergic receptors and may have different modes of action from that of standard neuroleptics.
Niwa
M
M
Department of Pharmacology, Gifu University School of Medicine.
Mibu
H
H
Nozaki
M
M
Tsurumi
K
K
Fujimura
H
H
D000818:Animals; D001058:Apomorphine / Q000008:administration & dosage; D001599:Berberine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D002164:Camphor / Q000494:pharmacology*; D002746:Chlorpromazine / Q000008:administration & dosage / Q000494:pharmacology; D003975:Diazepam / Q000008:administration & dosage / Q000494:pharmacology; D004338:Drug Combinations; D008297:Male; D008409:Mastication / Q000187:drug effects; D051379:Mice; D008815:Mice, Inbred Strains; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D012890:Sleep / Q000187:drug effects; D014316:Tritium
D004338:Drug Combinations; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D001599:Berberine; D014316:Tritium; D002164:Camphor; C048871:1-tetrahydroberberine, camphor sulfonate drug combination; D001058:Apomorphine; D003975:Diazepam; D002746:Chlorpromazine; C004645:canadine