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receptor ligands, enzyme inhibitors, signaling tools, ion channel modulators

Widely used, selective and competitive NMDA receptor antagonist which binds at glutamate site. More active form of DL-AP5. Blocks induction of LTP (long term potentiation) and impairs spatial learning.

Potent, selective and reversible, voltage dependent Na⁺ channel blocker. Use dependent. Citrate Salt. Commonly used in electrophysiological preparations to block or reduce excitability.

Clozapine N-oxide (CNO) is the prototypical chemical actuator for G_q- DREADDs. It is a metabolite of the atypical antipsychotic clozapine.

‘Excitatory’ G_q- coupled) DREADDs:

CNO activates the excitatory G_q- coupled DREADDs: hM3Dq, hM1Dq and hM5Dq.

The hM3Dq DREADD is typically used for enhancing neuronal firing and activating (G_q- signaling in neuronal and non-neuronal cells.

‘Inhibitory’ (G_i- coupled) DREADDs:

CNO also activates the inhibitory hM4Di and hM2Di G_i-coupled DREADDs.

The hM4Di DREADD is the most commonly used inhibitory DREADD and is used for neuronal silencing.

Gs and β-arrestin coupled DREADDs:

CNO also activates the G_s- coupled DREADD (GsD) and the β-arrestin preferring DREADD: rM3Darr (Rq(R165L).

In the literature, CNO has been administered intraperitoneally (i.p.), subcutaneously, directly infused intracranially, via drinking water or osmotic mini-pump. See our Technical review (table 3) for example administration methods and doses.

Recent findings suggest that systemically administered CNO does not readily cross the blood-brain-barrier in vivo, and converts to clozapine which activates DREADDs. Care must be taken in experimental design and proper controls should be incorporated.