| pubmed-article:11821023 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C0028040 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C0205245 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C1261322 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:11821023 | lifeskim:mentions | umls-concept:C1880371 | lld:lifeskim |
| pubmed-article:11821023 | pubmed:issue | 2-3 | lld:pubmed |
| pubmed-article:11821023 | pubmed:dateCreated | 2002-1-31 | lld:pubmed |
| pubmed-article:11821023 | pubmed:abstractText | Two 5-substituted derivatives of nicotine (nicotinic acetylcholine receptor: K(i)=2.4 nM) were synthesized and evaluated: 5-bromonicotine (K(i)=6.9 nM) and 5-methoxynicotine (K(i)=14.3 nM). Despite their high affinity, neither 5-bromonicotine nor 5-methoxynicotine mimicked nicotine in producing antinociceptive (tail-flick, hotplate), hypolocomotor, or hypothermic effects in mice. Neither agent antagonized the hypolocomotor actions of nicotine, whereas 5-methoxynicotine, but not 5-bromonicotine, antagonized the antinociceptive (tail-flick) activity of nicotine in a dose-related manner. In tests of stimulus generalization using rats trained to discriminate 0.6 mg/kg of (-)-nicotine from vehicle, 5-bromonicotine substituted for nicotine. Further evaluation of 5-bromonicotine indicated that it might be a partial agonist at alpha4beta2 receptors (stimulation of Rb(+) efflux; alpha4beta2 receptors expressed in oocytes) and at alpha3-containing nicotinic acetylcholine receptors (synaptosomal dopamine release). Thus, 5-bromonicotine might be acting as a partial agonist at alpha4beta2 receptors and/or some of its effects might be related to interactions with non-alpha4beta2 receptors. Clearly, the effects of 5-bromonicotine and 5-methoxynicotine are different from those of nicotine, and from one another. These actions demonstrate that substitution at the 5-position of nicotine exerts a profound influence on the pharmacological profile as well as agonist/antagonist properties of nicotine. | lld:pubmed |
| pubmed-article:11821023 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:language | eng | lld:pubmed |
| pubmed-article:11821023 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11821023 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:11821023 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:11821023 | pubmed:issn | 0014-2999 | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:DukatMa?gorza... | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:GlennonRichar... | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:MartinBilly... | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:YoungRichardR | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:DamajImad MIM | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:VannRobertR | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:CollinsAllan... | lld:pubmed |
| pubmed-article:11821023 | pubmed:author | pubmed-author:MarksMichael... | lld:pubmed |
| pubmed-article:11821023 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:11821023 | pubmed:day | 25 | lld:pubmed |
| pubmed-article:11821023 | pubmed:volume | 435 | lld:pubmed |
| pubmed-article:11821023 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:11821023 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:11821023 | pubmed:pagination | 171-80 | lld:pubmed |
| pubmed-article:11821023 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
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| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:meshHeading | pubmed-meshheading:11821023... | lld:pubmed |
| pubmed-article:11821023 | pubmed:year | 2002 | lld:pubmed |
| pubmed-article:11821023 | pubmed:articleTitle | Functional diversity among 5-substituted nicotine analogs; in vitro and in vivo investigations. | lld:pubmed |
| pubmed-article:11821023 | pubmed:affiliation | Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Box 980540 VCU, Richmond, VA 23298-0540, USA. mdukat@hsc.vcu.edu | lld:pubmed |
| pubmed-article:11821023 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:11821023 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
