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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
14
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pubmed:dateCreated |
1994-8-18
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pubmed:abstractText |
The synthesis of 5-(arylacetyl)-4-[(alkylamino)methyl]furo[3,2-c] pyridines (16-23, 26, 27) and their activities as kappa-opioid receptor agonists are described. kappa-Agonist potency was particularly sensitive to the nature of the basic moiety. In particular, in the rabbit vas deferens (kappa-specific tissue), the 3-pyrrolidinol analogue 17 (IC50 = 2.7 nM) was found to be approximately 5-fold more potent than the corresponding pyrrolidine analogue 16 (IC50 = 15 nM). In the rat and hamster vasa deferentia (mu-specific and delta-specific tissues, respectively), 17 showed only weak antagonist activity (pKB > 5.5), underlining its selectivity for the kappa-opioid receptor. The major activity for 17 is resident in the 4S,3'S-isomer 26 (rabbit vas deferens IC50 = 1.1 nM). Compound 26 displays excellent antinociceptive activity, as determined in the mouse acetylcholine-induced abdominal constriction test (ED50 = 0.001 mg/kg, sc).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
8
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pubmed:volume |
37
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
2138-44
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8035420-Analgesics,
pubmed-meshheading:8035420-Animals,
pubmed-meshheading:8035420-Cricetinae,
pubmed-meshheading:8035420-Male,
pubmed-meshheading:8035420-Mice,
pubmed-meshheading:8035420-Narcotics,
pubmed-meshheading:8035420-Pyridines,
pubmed-meshheading:8035420-Rabbits,
pubmed-meshheading:8035420-Rats,
pubmed-meshheading:8035420-Receptors, Opioid, kappa,
pubmed-meshheading:8035420-Stereoisomerism,
pubmed-meshheading:8035420-Vas Deferens
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pubmed:year |
1994
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pubmed:articleTitle |
4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware, Hertfordshire, England.
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pubmed:publicationType |
Journal Article,
In Vitro
|