Binding of an imidazopyridoindole at imidazoline I2 receptors.
3,5,6,11-Tetrahydro-2H-imidazo[1',2':1,2]pyrido[3,4-b]indole (10) might be viewed as a fusion structure of two classes of I(2) imidazoline receptor ligands: 2-(2-benzofuranyl)-2-imidazolines and beta-carbolines. Its high affinity (K(i)=7.3 nM) provides insight to how the two classes of agents might bind relative to one another at I(2) receptors.
Glennon
Richard A
RA
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA. glennon@hsc.vcu.edu
Grella
Brian
B
Tyacke
Robin J
RJ
Lau
Alice
A
Westaway
Julie
J
Hudson
Alan L
AL
D000818:Animals; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism*; D054755:Imidazoline Receptors; D007211:Indoles / Q000737:chemistry / Q000378:metabolism*; D008297:Male; D011485:Protein Binding / Q000502:physiology; D011728:Pyridones / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011955:Receptors, Drug / Q000378:metabolism*
D007093:Imidazoles; D054755:Imidazoline Receptors; D007211:Indoles; D011728:Pyridones; D011955:Receptors, Drug; C029899:imidazole