2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.
A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD2 receptors can be controlled by suitable C-2 aryl groups.
Stevenson
G I
GI
Merck Sharp & Dohme Research Laboratories, Thle Neuroscience Research Centre, Harlow, Essex, UK. graeme_stevenson@merck.com
Smith
A L
AL
Lewis
S
S
Michie
S G
SG
Neduvelil
J G
JG
Patel
S
S
Marwood
R
R
Patel
S
S
Castro
J L
JL
D000818:Animals; D001667:Binding, Competitive; D006801:Humans; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000138:chemical synthesis / Q000494:pharmacology*
D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines