Document Detail

Interaction of orally administered 5-[3-[((2S)-1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxole (MKC-242) with 5-HT1A receptors in rat brain.
MedLine Citation:
PMID:  9195299     Owner:  NLM     Status:  MEDLINE    
The present study was carried out to clarify whether orally administered 5-{3-[((2S)-1,4-benzodioxan-2-ylmethyl)amino]propoxy}-1,3-be nzodioxole (MKC-242), a serotonin1A (5-HT1A)-receptor agonist having potent anxiolytic-like and antidepressant-like effects in animal models, binds to 5-HT1A receptors in rat brain. Quantitative autoradiography showed that orally administered MKC-242 (0.1-0.5 mg/kg) caused a significant decrease in 3[H]8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) binding in the hippocampus and dorsal raphe nucleus sections. The decrease in the binding by MKC-242 was observed up to 4 hr after administration, and the effective doses were similar to those in its anxiolytic-like effect in the animal models. Repeated treatment of MKC-242 (0.5 mg/kg/day, p.o.) or buspirone (30 mg/kg/day, p.o.) for 2 weeks did not affect [3H]8-OH-DPAT binding in both sections. These results suggest that orally administered MKC-242 at the low doses that do not show 5-HT1A-receptor-mediated in vivo responses such as the hypothermic effect, adrenocortical effect and the decrease in 5-HT turnover passes the blood-brain barrier and subsequently binds to 5-HT1A receptors in rat brain. In addition, they indicate that repeated stimulation of the receptors by the agonists does not affect the number of the binding sites.
S Asano; T Matsuda; T Yoshikawa; P Somboonthum; H Tasaki; M Abe; A Baba
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Japanese journal of pharmacology     Volume:  74     ISSN:  0021-5198     ISO Abbreviation:  Jpn. J. Pharmacol.     Publication Date:  1997 May 
Date Detail:
Created Date:  1997-08-05     Completed Date:  1997-08-05     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2983305R     Medline TA:  Jpn J Pharmacol     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  69-75     Citation Subset:  IM    
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Osaka University, Japan.
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MeSH Terms
5,7-Dihydroxytryptamine / pharmacology
8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacokinetics,  pharmacology
Binding, Competitive / drug effects
Brain / anatomy & histology,  drug effects
Brain Chemistry / drug effects*
Dioxanes / pharmacokinetics,  pharmacology*
Dioxoles / pharmacokinetics,  pharmacology*
Neurons / drug effects
Rats, Wistar
Receptors, Serotonin / drug effects,  metabolism*
Serotonin / physiology
Serotonin Agents / pharmacology
Serotonin Agonists / pharmacokinetics,  pharmacology*
Reg. No./Substance:
0/Dioxanes; 0/Dioxoles; 0/MKC 242; 0/Receptors, Serotonin; 0/Serotonin Agents; 0/Serotonin Agonists; 31363-74-3/5,7-Dihydroxytryptamine; 50-67-9/Serotonin; 78950-78-4/8-Hydroxy-2-(di-n-propylamino)tetralin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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