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A series of (8 beta)-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid cycloalkyl esters were prepared and examined for blockade of vascular 5HT2 receptors. The antagonist in this series that had the highest 5HT2 receptor affinity was (8 beta)-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid cyclohexyl ester. This compound was therefore chosen as the basic backbone of a structure-activity study to determine what effect different N1-substituents, N6-substituents, and ester ring substituents had on 5HT2 receptor affinity. Maximal 5HT2 receptor affinity was obtained when the N1-substituent was isopropyl, the N6-substituent was methyl, and there was a hydroxy or keto substituent in the 4-position of the ester cyclohexyl ring.
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
July 1990,
Journal of medicinal chemistry,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
January 1979,
NIDA research monograph,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
April 2012,
Bioorganic & medicinal chemistry,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
August 1956,
Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
May 2013,
Bioorganic & medicinal chemistry,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
February 1982,
Acta pharmacologica et toxicologica,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
August 2008,
Journal of enzyme inhibition and medicinal chemistry,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
August 2007,
Bioorganic & medicinal chemistry letters,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
February 1968,
Experientia,
W L Garbrecht, and
G Marzoni, and
K R Whitten, and
M L Cohen
June 1982,
Neuropharmacology,
