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In Vitro Properties of a High Affinity Selective Antagonist of the VIP1 Receptor
Lab study of a strong and selective blocker for the VIP1 receptor
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Abstract
The IC50 values of the new selective VIP1 receptor antagonist PG 97-269 were 10 nM for rat VIP1 receptors and 3000 nM for human VIP2 receptors.
- PG 97-269 shows high selectivity for the VIP1 receptor subclass compared to other receptors.
- It inhibits the binding of a labeled VIP peptide, indicating its potential as an effective antagonist.
- The compound does not stimulate adenylate cyclase activity but inhibits VIP-mediated stimulation of this enzyme.
- Ki values were determined to be 15 +/- 5 nM for rat VIP1 receptors and 2 +/- 1 nM for human VIP1 receptors.
- PG 97-269 has negligible affinity for the PACAP I receptor type.
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