Source:http://linkedlifedata.com/resource/pubmed/id/11323234
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2001-4-27
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pubmed:abstractText |
To diagnose and investigate neurodegenerative diseases affecting cholinergic neuron density, piperazine derivatives of vesamicol were synthesized and evaluated. Previously, we reported that trans-5-iodo-2-hydroxy-3-[4-phenylpiperazinyl] tetralin (DRC140, 1) possessed high selectivity for vesicular acetylcholine transporter (VAChT). In present study of the effect of alkyl substituents, we observed that the introduction of a methyl group into the ortho or meta positions of the phenyl group of 1 increased affinity for VAChT. trans-5-Iodo-2-hydroxy-3-[4-[2-methylphenyl] piperazinyl]tetralin (2) displayed high affinity and specificity for VAChT. The regional distributions of radioactivity in the rat brain correlated well with known patterns of central cholinergic innervation. [(123)I]2 is a potentially useful compound for SPECT imaging.
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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 |
Apr
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pubmed:issn |
0969-8051
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
28
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
251-60
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:11323234-Animals,
pubmed-meshheading:11323234-Autoradiography,
pubmed-meshheading:11323234-Brain,
pubmed-meshheading:11323234-Cholinergic Fibers,
pubmed-meshheading:11323234-Chromatography, High Pressure Liquid,
pubmed-meshheading:11323234-Guinea Pigs,
pubmed-meshheading:11323234-Male,
pubmed-meshheading:11323234-Neuromuscular Depolarizing Agents,
pubmed-meshheading:11323234-Neurons,
pubmed-meshheading:11323234-Piperidines,
pubmed-meshheading:11323234-Radiopharmaceuticals,
pubmed-meshheading:11323234-Rats,
pubmed-meshheading:11323234-Rats, Wistar,
pubmed-meshheading:11323234-Structure-Activity Relationship,
pubmed-meshheading:11323234-Tissue Distribution,
pubmed-meshheading:11323234-Tomography, Emission-Computed, Single-Photon
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pubmed:year |
2001
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pubmed:articleTitle |
Synthesis and evaluation of radiolabeled piperazine derivatives of vesamicol as SPECT agents for cholinergic neurons.
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pubmed:affiliation |
Research Center, Daiichi Radioisotope Laboratories, LTD., 453-1, Shimo-Okura, Matsuo-Machi, Sanbu-Gun, 289-1592, Chiba, Japan. bkazunori@drl.co.jp
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pubmed:publicationType |
Journal Article
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