- Purine derivatives
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A compound of formula (I), or a pharmaceutically acceptable salt thereof: STR1 wherein X is hydrogen, amino, halogen, hydroxy, lower alkoxy or lower alkyl andR 1 is STR2 wherein Y is methylene or a valence bond, R 2 and R 5 is H or lower, straight or branched alkyl,R 3 is H or lower alkyl, orR 2 and R 3 can together form a cyclobutyl, cyclopentyl, cyclohexyl or phenyl ring,Z is oxygen, methylene, sulphur, sulphonyl or a valence bond,R 4 is H, lower alkyl, aralkyl, a mono or bicyclic aromatic system optionally substituted with various groups.The compounds have been found useful for treating central nervous system ailments.
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- Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.
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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,Secunda,Daly,Olsson
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p. 3388 - 3390
(2007/10/02)
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