rdf:type |
|
lifeskim:mentions |
umls-concept:C0013030,
umls-concept:C0030685,
umls-concept:C0034830,
umls-concept:C0086597,
umls-concept:C0175815,
umls-concept:C0205314,
umls-concept:C0243076,
umls-concept:C0391871,
umls-concept:C0679622,
umls-concept:C0680255,
umls-concept:C1283071,
umls-concept:C1705542,
umls-concept:C1963578
|
pubmed:issue |
24
|
pubmed:dateCreated |
2007-11-16
|
pubmed:abstractText |
A series of tris-azaaromatic quaternary ammonium salts has been synthesized and evaluated for their ability to inhibit neuronal nicotinic acetylcholine receptors (nAChRs) mediating nicotine-evoked [(3)H]dopamine release from superfused rat striatal slices and for inhibition of [(3)H]nicotine and [(3)H]methyllycaconitine binding to whole rat brain membranes. The 3-picolinium compound 1,3,5-tri-{5-[1-(3-picolinium)]-pent-1-ynyl}benzene tribromide (tPy3PiB), 3b, exhibited high potency and selectivity for nAChR subtypes mediating nicotine-evoked [(3)H]dopamine release with an IC(50) of 0.2 nM and I(max) of 67%.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
1464-3405
|
pubmed:author |
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
17
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
6701-6
|
pubmed:meshHeading |
pubmed-meshheading:17977723-Animals,
pubmed-meshheading:17977723-Aza Compounds,
pubmed-meshheading:17977723-Brain,
pubmed-meshheading:17977723-Dopamine,
pubmed-meshheading:17977723-Molecular Structure,
pubmed-meshheading:17977723-Nicotine,
pubmed-meshheading:17977723-Nicotinic Antagonists,
pubmed-meshheading:17977723-Quaternary Ammonium Compounds,
pubmed-meshheading:17977723-Rats,
pubmed-meshheading:17977723-Receptors, Nicotinic,
pubmed-meshheading:17977723-Salts,
pubmed-meshheading:17977723-Structure-Activity Relationship,
pubmed-meshheading:17977723-Tromethamine
|
pubmed:year |
2007
|
pubmed:articleTitle |
Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
|
pubmed:affiliation |
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
|