Heterogeneity of imidazoline binding sites revealed by a cirazoline derivative.
The affinity of AMPI (2-[3-aminophenoxy]methyl imidazoline) for [3H]clonidine and [3H]idazoxan imidazoline binding sites was determined in various rabbit and human tissues. Although cirazoline showed a high affinity (nM range) in all the tested tissues, its derivative, AMPI, had a high affinity (nM range) in rabbit brain and kidney but a low affinity (microM range) in the human brain. These differences in affinities were very similar to those obtained with amiloride. The same results were obtained when considering [3H]clonidine or [3H]idazoxan specific imidazoline binding sites.
Greney
H
H
CNRS URA 589, Faculté de Médecine, Université Louis Pasteur, Strasbourg, France.
Molines
A
A
Bousquet
P
P
Dontenwill
M
M
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D003000:Clonidine / Q000378:metabolism*; D004146:Dioxanes / Q000378:metabolism*; D006801:Humans; D019329:Idazoxan; D007093:Imidazoles / Q000378:metabolism*; D054755:Imidazoline Receptors; D007668:Kidney / Q000378:metabolism; D011817:Rabbits; D011955:Receptors, Drug / Q000378:metabolism*; D013045:Species Specificity
D004146:Dioxanes; D007093:Imidazoles; D054755:Imidazoline Receptors; D011955:Receptors, Drug; C058215:2-amino-1-methyl-5-propylideneimidazol-4-one; D003000:Clonidine; D019329:Idazoxan