Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K(i)=3nM) indicates that the indolic nitrogen atom is not essential for binding.
Kolanos
Renata
R
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA.
Siripurapu
Uma
U
Pullagurla
Manik
M
Riaz
Mohamed
M
Setola
Vince
V
Roth
Bryan L
BL
Dukat
Małgorzata
M
Glennon
Richard A
RA
D001665:Binding Sites; D006801:Humans; D007192:Indenes / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D011985:Receptors, Serotonin / Q000737:chemistry / Q000378:metabolism*; D014363:Tryptamines / Q000737:chemistry / Q000378:metabolism*
D007192:Indenes; D011985:Receptors, Serotonin; D014363:Tryptamines; C097216:serotonin 6 receptor