Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives

1983 ◽  
Vol 26 (3) ◽  
pp. 436-439 ◽  
Author(s):  
K. Seamon ◽  
J. W. Daly ◽  
H. Metzger ◽  
N. J. De Souza ◽  
J. Reden
Keyword(s):  
Adenylate Cyclase ◽  
Structure Activity Relationships ◽  
Structure Activity

Definition of subclasses of adenosine receptors associated with adenylate cyclase: interaction of adenosine analogs with inhibitory A1 receptors and stimulatory A2 receptors

1987 ◽  
Vol 65 (3) ◽  
pp. 365-376 ◽  
Author(s):  
Dieter Ukena ◽  
Ray A. Olsson ◽  
John W. Daly
Keyword(s):  
Adenylate Cyclase ◽  
Adenosine Receptors ◽  
Cell Types ◽  
Structural Heterogeneity ◽  
Human Platelets ◽  
Pharmacological Characterization ◽  
Structure Activity Relationships ◽  
Adenosine Analogs ◽  
Structure Activity ◽  
Definition Of

The structure–activity relationships of 63 adenosine analogs as agonists for the A1 adenosine receptors that mediate inhibition of adenylate cyclase activity in rat fat cells and for the A2 adenosine receptors that mediate stimulation of adenylate cyclase in rat pheochromocytoma PC12 cells and human platelets were determined. The lack of correspondence between the structure–activity relationships of these analogs at the A1 and A2 receptors appear definitive in terms of establishing the existence of A1 and A2 subclasses of adenosine receptors. However, significant differences in the agonist profiles at A2 receptors of platelet and PC12 indicate a certain degree of structural heterogeneity within the members of the A2 adenosine receptor subclass. Whether such differences are due to different species or different cell types is not known. A set of adenosine analogs, such as N6-cyclohexyl-, N6-R-, and S-1-phenyl-2- propyladenosines, 5′-N-ethylcarboxamidoadenosine and its N6-cyclohexyl derivative, 2-chloro- adenosine, and 2-phenylaminoadenosine, appear to represent a series of analogs useful for pharmacological characterization of A1 and A2 classes of adenosine receptors.

Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
Q Do ◽  
H Doan Thi Mai ◽  
T Gaslonde ◽  
B Pfeiffer ◽  
S Léonce ◽  
...  
Keyword(s):  
Pyran Ring ◽  
Structure Activity Relationships ◽  
Structure Activity
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