PMID- 9535013
OWN - NLM
STAT- MEDLINE
DCOM- 19980513
LR  - 20220823
IS  - 0007-1188 (Print)
IS  - 0007-1188 (Linking)
VI  - 123
IP  - 5
DP  - 1998 Mar
TI  - Effect of gamma-mangostin through the inhibition of 5-hydroxy-tryptamine2A 
      receptors in 5-fluoro-alpha-methyltryptamine-induced head-twitch responses of 
      mice.
PG  - 855-62
AB  - 1. Intracerebronventricular (i.c.v.) injection of gamma-mangostin (10-40 
      nmol/mouse), a major compound of the fruit hull of Garcinia mangostana Lin., like 
      ketanserin (10, 20 nmol/mouse, i.c.v.) inhibited 5-fluoro-alpha-methyltryptamine 
      (5-FMT) (45 mg kg(-1), i.p.)-induced head-twitch response in mice in the presence 
      or absence of citalopram (a 5-hydroxytryptamine (5-HT)-uptake inhibitor). 2. 
      Neither the 5-FMT- nor the 8-hydroxy-2-(di-n-propylamino)tetralin 
      (5-HT1A-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was 
      affected by gamma-mangostin or ketanserin. 3. The locomotor activity stimulated 
      by 5-FMT through the activation of alpha1-adrenoceptors did not alter in the 
      presence of gamma-mangostin. 4. 5-HT-induced inositol phosphates accumulation in 
      mouse brain slices was abolished by ketanserin. Gamma-mangostin caused a 
      concentration-dependent inhibition of the inositol phosphates accumulation. 5. 
      Gamma-mangostin caused a concentration-dependent inhibition of the binding of 
      [3H]-spiperone, a specific 5-HT2A receptor antagonist, to mouse brain membranes. 
      6. Kinetic analysis of the [3H]-spiperone binding revealed that gamma-mangostin 
      increased the Kd value without affecting the Bmax value, indicating the mode of 
      the competitive nature of the inhibition by gamma-mangostin. 7. These results 
      suggest that gamma-mangostin inhibits 5-FMT-induced head-twitch response in mice 
      by blocking 5-HT2A receptors not by blocking the release of 5-HT from the central 
      neurone. Gamma-mangostin is a promising 5-HT2A receptor antagonist in the central 
      nervous system.
FAU - Chairungsrilerd, N
AU  - Chairungsrilerd N
AD  - Department of Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku 
      University, Sendai, Japan.
FAU - Furukawa, K
AU  - Furukawa K
FAU - Tadano, T
AU  - Tadano T
FAU - Kisara, K
AU  - Kisara K
FAU - Ohizumi, Y
AU  - Ohizumi Y
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Br J Pharmacol
JT  - British journal of pharmacology
JID - 7502536
RN  - 0 (Inositol Phosphates)
RN  - 0 (Receptor, Serotonin, 5-HT2A)
RN  - 0 (Receptors, Serotonin)
RN  - 0 (Serotonin Antagonists)
RN  - 0 (Tryptamines)
RN  - 0 (Xanthenes)
RN  - 0 (Xanthones)
RN  - 4X6E73CJ0Q (Spiperone)
RN  - 712-08-3 (5-fluoro-alpha-methyltryptamine)
RN  - 78950-78-4 (8-Hydroxy-2-(di-n-propylamino)tetralin)
RN  - 97F9DE4CT4 (Ketanserin)
RN  - U6RIV93RU1 (mangostin)
SB  - IM
MH  - 8-Hydroxy-2-(di-n-propylamino)tetralin/pharmacology
MH  - Animals
MH  - Brain/metabolism
MH  - Injections, Intraventricular
MH  - Inositol Phosphates/metabolism
MH  - Ketanserin/pharmacology
MH  - Male
MH  - Mice
MH  - Motor Activity/*drug effects
MH  - Radioligand Assay
MH  - Receptor, Serotonin, 5-HT2A
MH  - Receptors, Serotonin/*drug effects
MH  - Serotonin Antagonists/administration & dosage/*pharmacology
MH  - Spiperone/metabolism
MH  - Tryptamines/*pharmacology
MH  - Xanthenes/administration & dosage/*pharmacology
MH  - *Xanthones
PMC - PMC1565246
EDAT- 1998/04/16 00:00
MHDA- 1998/04/16 00:01
PMCR- 1999/03/01
CRDT- 1998/04/16 00:00
PHST- 1998/04/16 00:00 [pubmed]
PHST- 1998/04/16 00:01 [medline]
PHST- 1998/04/16 00:00 [entrez]
PHST- 1999/03/01 00:00 [pmc-release]
AID - 0701695 [pii]
AID - 10.1038/sj.bjp.0701695 [doi]
PST - ppublish
SO  - Br J Pharmacol. 1998 Mar;123(5):855-62. doi: 10.1038/sj.bjp.0701695.