TY - JOUR
T1 - A novel analogue of clonidine with opiate-receptor agonist activity
AU - Atlas, Daphna
AU - Sabol, Steven L.
PY - 1980/6/16
Y1 - 1980/6/16
N2 - A new analogue of the α2-adrenergic receptor ligand clonidine, N-(4-hydroxphenacetyl)-4-aminoclonidine, was synthesized. The analogue possesses opiate-receptor agonist activity in addition to α-adrenergic partial agonist activity. The analogue elicits inhibition of adenylate cyclase of NG108-15 neuroblastoma × glioma hybrid cells; most of the inhibition is reversed by the opiate-receptor antagonist naloxone. The analogue also inhibits the binding of [3H]D-Ala2-Met5-enkephalinamide and [3H]dihydromorphine to rat brain opiate receptors. The structure of the analogue suggests common elements in the ligand binding sites of α- and opiate receptors and may lead to a new class of opiate analgesics.
AB - A new analogue of the α2-adrenergic receptor ligand clonidine, N-(4-hydroxphenacetyl)-4-aminoclonidine, was synthesized. The analogue possesses opiate-receptor agonist activity in addition to α-adrenergic partial agonist activity. The analogue elicits inhibition of adenylate cyclase of NG108-15 neuroblastoma × glioma hybrid cells; most of the inhibition is reversed by the opiate-receptor antagonist naloxone. The analogue also inhibits the binding of [3H]D-Ala2-Met5-enkephalinamide and [3H]dihydromorphine to rat brain opiate receptors. The structure of the analogue suggests common elements in the ligand binding sites of α- and opiate receptors and may lead to a new class of opiate analgesics.
UR - http://www.scopus.com/inward/record.url?scp=0019314026&partnerID=8YFLogxK
U2 - 10.1016/0006-291X(80)91323-6
DO - 10.1016/0006-291X(80)91323-6
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C2 - 6249294
AN - SCOPUS:0019314026
SN - 0006-291X
VL - 94
SP - 924
EP - 931
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 3
ER -