I2 imidazoline ligand
I2 imidazoline binding-site ligand
- I2 sites: an allosteric region on monoamine oxidase
- On MAO-B; not a classical receptor
- Modulates monoamine metabolism
- A role in pain signaling
- Binding is well described; the clinical effect is not
Drugs with this mechanism (4)
- Clonidine — Central alpha-2 agonist for hypertension, ADHD and withdrawal; sedation and rebound.
- Clonidine ER — Extended-release central alpha-2 agonist for ADHD; sedation and rebound hypertension limit it.
- Clonidine ER suspension — Extended-release clonidine liquid for ADHD; sedation and rebound hypertension shape use.
- Tizanidine — Short-acting alpha-2 agonist for spasticity; hypotension and CYP1A2 interactions.
Self-check
- Are I2 imidazoline sites classical receptors?
No; they are sites on MAO-B. - How established is the clinical effect of I2 binding?
Binding is well described; the clinical effect is not.
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