BU98008, a highly selective imidazoline(1)-receptor ligand.
BU98008 (1-(4, 5-dihydro-1H-imidazol-2-yl)isoquinoline) is a novel isoquinoline derivative. Radioligand binding studies revealed it had high affinity for the I(1) receptor in rat kidney membranes but low affinity for the I(2) binding site and alpha(2)-adrenoceptor in rat brain membranes. Further evaluation of BU98008 in vivo revealed no effect on blood pressure following peripheral administration. These preliminary data suggest BU98008 may be an antagonist at I(1) receptors. Further evaluation following central administration must be performed before a hypotensive action can be excluded.
Robinson
E S J
ES
Psychopharmacology Unit, School of Medical Sciences, Bristol BS8 1TD, UK.
Price
R E
RE
Nutt
D J
DJ
Hudson
A L
AL
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D001921:Brain / Q000166:cytology / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D003000:Clonidine / Q000494:pharmacology; D006339:Heart Rate / Q000187:drug effects; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D054755:Imidazoline Receptors; D007546:Isoquinolines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D007668:Kidney / Q000166:cytology / Q000378:metabolism; D008024:Ligands; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D011918:Rats, Inbred SHR; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D011955:Receptors, Drug / Q000037:antagonists & inhibitors / Q000378:metabolism*
C483907:1-(4,5-dihydro-1H-imidazol-2-yl)isoquinoline; D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D054755:Imidazoline Receptors; D007546:Isoquinolines; D008024:Ligands; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug; C410887:imidazoline I1 receptors; D003000:Clonidine