Constitutive Activity
The ability of a receptor to produce a biological response in the absence of a bound agonist. Some receptors exist in a spontaneous active conformation, generating basal signaling. Inverse agonists reduce constitutive activity below baseline, while neutral antagonists block agonist binding without affecting basal activity.
例
- Histamine H3 receptor shows constitutive activity (inverse agonist: pitolisant)
- Wild-type cannabinoid CB1 receptor constitutive activity
- Mutant TSH receptor constitutive activity in hyperthyroidism
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The ability of a receptor to produce a biological response in the absence of a bound agonist. Some receptors exist in a spontaneous active conformation, generating basal signaling. Inverse agonists …