Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.
Radioligand binding studies of N6-substituted adenosines at the A1 and A2 adenosine receptors of rat brain cortex and rat brain striatum, respectively, show that a 2-chloro substituent does not consistently change the affinity or the selectivity of these analogues for the A1 receptor. A 2-chloro substituent lowers the characteristic stereoselectivity of the A1 receptor toward the R diastereomer of N6-(1-phenyl-2-propyl)adenosine. A 2-chloro substituent consistently increases potency of N6-substituted adenosines as agonists at an adenosine A2 receptor stimulatory to adenylate cyclase in PC12 cell membranes.
Thompson
R D
RD
Department of Internal Medicine, University of South Florida, Tampa 33612.
Secunda
S
S
Daly
J W
JW
Olsson
R A
RA
D015762:2-Chloroadenosine / Q000031:analogs & derivatives* / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000378:metabolism; D066298:In Vitro Techniques; D051381:Rats; D011983:Receptors, Purinergic / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011983:Receptors, Purinergic; D015762:2-Chloroadenosine