- Agonists
- Apraclonidine
- Brimonidine
- Clonidine
- Detomidine
- Dexmedetomidine
- Guanabenz
- Guanfacine
- Lofexidine
- Medetomidine
- Romifidine
- Tizanidine
- Tolonidine
- Xylazine
- Fadolmidine
- Xylometazoline
- Oxymetazoline (partial α2 agonist)
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- Antagonists
- Atipamezole
- Cirazoline
- Efaroxan
- Idazoxan
- Mianserin
- Mirtazapine
- Napitane
- Phenoxybenzamine
- Phentolamine
- Rauwolscine
- Setiptiline
- Tolazoline
- Yohimbine
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