title: Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.
abstract: 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.
authors.affiliation: Department of Internal Medicine, University of South Florida, Tampa 33612.
authors.forename: R D
authors.initials: RD
authors.lastname: Thompson
authors.forename: S
authors.initials: S
authors.lastname: Secunda
authors.forename: J W
authors.initials: JW
authors.lastname: Daly
authors.forename: R A
authors.initials: RA
authors.lastname: Olsson
mesh_terms: 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
chemical_list: D011983:Receptors, Purinergic; D015762:2-Chloroadenosine