TY - JOUR
T1 - Quantitative structure - Activity relationship study on tetrahydro-β-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus
AU - Singh, P.
AU - Kumar, Rajesh
PY - 2001/12
Y1 - 2001/12
N2 - The antagonist actions of three sub-series of tetrahydro-β-carbolines at the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT2B receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.
AB - The antagonist actions of three sub-series of tetrahydro-β-carbolines at the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT2B receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.
KW - Antagonists
KW - Physicochemical properties
KW - QSAR analysis
KW - Serotonin 2B (5HT) contractile receptor
KW - Tetrahydro-β-carboline antagonists
UR - http://www.scopus.com/inward/record.url?scp=0035544951&partnerID=8YFLogxK
U2 - 10.1080/14756360127570
DO - 10.1080/14756360127570
M3 - ???researchoutput.researchoutputtypes.contributiontojournal.article???
C2 - 12164388
AN - SCOPUS:0035544951
SN - 8755-5093
VL - 16
SP - 491
EP - 497
JO - Journal of Enzyme Inhibition
JF - Journal of Enzyme Inhibition
IS - 6
ER -