Effects of sesquiterpenoids from "Oriental incenses" on acetic acid-induced writhing and D2 and 5-HT2A receptors in rat brain.
Six sesquiterpenoids, namely jinkoh-eremol, agarospirol, alpha- and beta-santalols, dehydrocostus lactone and costunolide, isolated from oriental incenses inhibited acetic acid-induced writhing in mice. The incidence of writhing produced by jinkoh-eremol, alpha-santalol and costunolide were revealed by administration of naloxone (mu-, kappa- and delta-antagonists). Inhibitory activities of alpha-santalol on opioid receptors were shown only by the delta antagonist, but not by the mu- and kappa-antagonists. The delta2-antagonist, but not the delta-antagonist, inhibited the activity of alpha santalol. The mechanism of inhibitory activity on the opioid receptor by alpha-santalol was different from that of morphine. Alpha-santalol was shown to be the most potent of the six as an antagonist of dopamine D2 and serotonine 5-HT2A receptor binding. The effect of alpha-santalol, was the same as that of chlorpromazine as an antipsychotic agent, although alpha-santalol was less potent than chlorpromazine.
Okugawa
H
H
Institute for Oriental Medicine, Hyogo, Amagasaki, Hyogo, Japan.
Ueda
R
R
Matsumoto
K
K
Kawanishi
K
K
Kato
K
K
D019342:Acetic Acid; D000700:Analgesics / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D007783:Lactones; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010146:Pain / Q000517:prevention & control*; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use; D000081223:Polycyclic Sesquiterpenes; D011869:Radioligand Assay; D011957:Receptors, Opioid / Q000187:drug effects*; D012717:Sesquiterpenes / Q000494:pharmacology / Q000627:therapeutic use*; D013141:Spiro Compounds; D013764:Tetrahydronaphthalenes
D000700:Analgesics; D007783:Lactones; D010936:Plant Extracts; D000081223:Polycyclic Sesquiterpenes; D011957:Receptors, Opioid; D012717:Sesquiterpenes; D013141:Spiro Compounds; D013764:Tetrahydronaphthalenes; C043206:santalol; C065858:hinesol; C083030:dehydrocostus lactone; C002602:costunolide; C101277:jinkoheremol; D019342:Acetic Acid