Initial evaluation of novel selective ligands for imidazoline(2) receptors in rat whole brain.
Indazim, the indazole analogue of 2BFI, and four methyl-substituted analogues were tested for their affinity at the imidazoline(2) binding site (I(2)-BS), and this affinity was compared with their affinity at the alpha(2)-adrenoceptor to determine their structure, affinity relationship, and selectivity at the I(2)-BS. These studies showed that these ligands were highly selective for the I(2)-BS compared with 2BFI and that substitution at the 4 and 7 positions increased affinity without affecting selectivity.
Tyacke
R J
RJ
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, UK.
Sazczewski
F
F
Tabin
P
P
Sazczewski
J
J
Nutt
D J
DJ
Hudson
A L
AL
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000166:cytology / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D054755:Imidazoline Receptors; D007191:Indazoles / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D008297:Male; D015394:Molecular Structure; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism*
D054755:Imidazoline Receptors; D007191:Indazoles; D008024:Ligands; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug