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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1983-12-17
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pubmed:abstractText |
Muscarinic acetylcholine receptors in the synaptic membrane fraction of porcine caudate nucleus were characterized by using a radiolabeled agonist, [3H]cis-methyldioxolane [( 3H]CD) and an antagonist, [3H]quinuclidinyl benzilate [( 3H]QNB). Scatchard analysis of the specific binding of [3H]CD gave a single equilibrium dissociation constant of 8.1 nM when a concentration of less than 80 nM [3H]CD was used. The binding capacity was 390 fmoles/mg of protein and corresponded to about 10% of the binding sites of [3H]QNB. Agonist/[3H]CD competition binding experiments indicated that [3H]CD was selectively bound to the sites with a high affinity for agonists. [3H]CD binding was inhibited by Na+, K+, Mg2+, and Ca2+ with the half-maximal effect at 10-50 mM. Nickel ion showed biphasic effects on [3H]CD binding: a 2- to 3-fold enhancement of binding at 0.1-10 mM and inhibition above 10 mM. Other cations, including Co2+, Mn2+, and Zn2+, at 1 mM also increased [3H]CD binding by a factor of 1.5-1.8. Among 18 cations examined, only Cd2+, Hg2+, and Cu2+ caused significant inhibition of [3H]CD binding at 1 mM. [3H]CD binding was decreased to about 20% of the control value in the presence of guanylyl-5'-imidodiphosphate (GppNHp), GTP, and GDP with the half-maximal effect at 1.3, 32, and 45 microM, respectively. [3H]CD binding in the presence of Ni2+ was decreased by GppNHp to a level obtained in the presence of GppNHp alone. The increase caused by Ni2+ in [3H]CD binding was due to the increase in the maximal binding capacity (Bmax) without changes in the affinity for [3H]CD. We conclude that Ni2+ increases the proportion of a muscarinic receptor subclass (or state) that is sensitive to guanyl nucleotide.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-methyldioxolane,
http://linkedlifedata.com/resource/pubmed/chemical/Cations,
http://linkedlifedata.com/resource/pubmed/chemical/Cations, Divalent,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxolanes,
http://linkedlifedata.com/resource/pubmed/chemical/Guanine Nucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Guanylyl Imidodiphosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Nickel,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidinyl Benzilate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0026-895X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
24
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
366-73
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6633503-Animals,
pubmed-meshheading:6633503-Binding, Competitive,
pubmed-meshheading:6633503-Cations,
pubmed-meshheading:6633503-Cations, Divalent,
pubmed-meshheading:6633503-Caudate Nucleus,
pubmed-meshheading:6633503-Dioxolanes,
pubmed-meshheading:6633503-Guanine Nucleotides,
pubmed-meshheading:6633503-Guanylyl Imidodiphosphate,
pubmed-meshheading:6633503-Nickel,
pubmed-meshheading:6633503-Quinuclidinyl Benzilate,
pubmed-meshheading:6633503-Receptors, Muscarinic,
pubmed-meshheading:6633503-Swine,
pubmed-meshheading:6633503-Synaptic Membranes
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pubmed:year |
1983
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pubmed:articleTitle |
Muscarinic receptors in porcine caudate nucleus. I. Enhancement by nickel and other cations of [3H]cis-methyldioxolane binding to guanyl nucleotide-sensitive sites.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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