scholarly journals Role of calmodulin in platelet aggregation. Structure-activity relationship of calmodulin antagonists.

1982 ◽  
Vol 69 (6) ◽  
pp. 1348-1355 ◽  
Author(s):  
M Nishikawa ◽  
H Hidaka
Keyword(s):  
Platelet Aggregation ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Calmodulin Antagonists ◽  
Structure Activity ◽  
Aggregation Structure ◽  
Relationship Of

Structure-Activity Relationship of the GPR55 Antagonist, CID16020046

Pharmacology ◽  
2018 ◽  
Vol 102 (5-6) ◽  
pp. 324-331 ◽  
Author(s):  
Andrew J. Brown ◽  
Irene Castellano-Pellicena ◽  
Carl P. Haslam ◽  
Paula L. Nichols ◽  
Simon J. Dowell
Keyword(s):  
Physiological Role ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Functional Responses ◽  
Mediated Effects ◽  
Structure Activity ◽  
Imaging Results ◽  
Relationship Of

Background/Aims: CID16020046 blocks the effect of the lipid lysophosphatidylinositol (LPI) at its receptor, GPR55. CID16020046 and another antagonist, ML193, have been used to investigate GPR55-mediated effects of LPI on cells, tissues, and in vivo. Here we describe the structure-activity relationship of CID16020046. Methods: Yeast or human cells were engineered to express GPR55 or control receptors. Cells were pretreated with a test agent before agonist challenge. Functional responses were quantified by yeast gene-reporter or calcium imaging. Results: Three substituents around the central pyrazololactam core of CID16020046 are each tolerant to substitution without abolishing GPR55 activity. Analogues of CID16020046 with potency at GPR55 ranging >1,000-fold are described, including several lacking activity up to the top concentration tested. One analogue, compound 1 (GSK875734A), has approximately 50-fold greater potency than CID16020046 in an inverse agonist assay. CID16020046, ML193 and 2 further antagonists (ML191 and ML192) all block the effect of a surrogate agonist at human GPR55. ML193, CID16020046 and several other examples of the pyrazololactam chemotype were also shown to antagonise rat GPR55. Conclusion: These data confirm the utility of CID16020046 and ML193 as tools to investigate the physiological role of GPR55, and offer starting points for GPR55 antagonists with optimised pharmacokinetic or other properties.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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