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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.

Water soluble, prototypical chemical actuator for Gq-DREADDs. Inert metabolite of the atypical antipsychotic clozapine.

Activates the G_i-DREADD receptors: hM3Dq, hM1Dq and hM5Dq. hM3Dq is typically used for enhancing neuronal firing and activating G_q- signaling in neuronal and non-neuronal cells.

CNO also activates the hM4Di and hM2Di G_q-DREADD receptors. The most commonly used inhibitory DREADD; hM4Di is used for neuronal silencing.

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

Clozapine N-oxide has rapid CNS penetration and distribution and allows minimally invasive delivery - CNO has been shown to be administered via drinking water, intraperitoneal injection or directly infused intracranially.