Multiple P2 receptor subtypes on platelets: a new interpretation of their function

Article Abstract:

Several studies have examined the influence of multiple P2 receptor subtypes on platelets. Results showed that the effects of ADP on platelets were correlated with a single receptor. However, the use of 2-substituted derivatives of ADP showed that the ADP receptor coupled to inhibition of adenylate class was different from the receptor influencing shape changes and aggregation. Moreover, findings of other studies suggested that some agonist-induced physiological responses may correlate with the simultaneous activation of multiple receptor subtypes by the same agonist.

Blood platelets, Adenosine diphosphate

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Quantitation of allosteric interactions

Article Abstract:

The equilibrium potency of allosteric agents may not be similar to their potency in dissociation assays. The same allosteric agent may exhibit different cooperativities with different ligands. If an allosteric agent is to be used in vivo, it will be essential to determine its affinity at the free receptor and its cooperativity with the endogenous agonist. This data cannot be gathered by using only a kinetic assay.

Allosteric proteins, Radioligand assay

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Endogenous ligands and inverse agonism

Article Abstract:

The existence of inverse agonists should remain speculative until reliable discriminatory criteria is formulated. Studies that attempted to directly measure levels of potential contaminating agonist have resulted in low levels of stimulation thereby making it difficult to assess ligand behavior. Thus, future studies should require greater appreciation of the pharmacological features of protean ligand behavior.

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