consciousness

Every compound in the sci-wiki that affects consciousness; the ones you can source are floated to the front, then the reference-only entries. Tap any for the full entry, mechanism, and outlets.

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Anesthetic

Hydroxydione

Hydroxydione is a synthetic pregnane neuroactive steroid that, introduced by Pfizer in 1955 under the trade name Viadril (also Presuren), became the first steroid used as an intravenous general anesthetic. The parent steroid, 21-hydroxy-5-beta-pregnane-3,20-dione, is almost insoluble in water; esterifying its 21-hydroxyl group with succinic acid and forming the sodium salt yields hydroxydione sodium succinate, a water-soluble prodrug that plasma esterases (enzymes that cleave ester bonds) hydrolyze in vivo to release the active steroid. Like later neurosteroid anesthetics such as alfaxalone, it produces hypnosis by acting as a positive allosteric modulator of the GABA-A receptor (the brain's principal inhibitory chloride ion channel), without meaningful analgesic or classical hormonal activity. Although valued for a wide margin of cardiovascular and respiratory safety, its very slow onset and a high incidence of injection-site thrombophlebitis (painful inflammation and clotting of the vein) led to its abandonment, yet it remains historically pivotal as the origin of the entire field of steroid anesthesia.

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Anesthetic

Org 21465

Org 21465 (also written ORG-21465) is a water-soluble aminosteroid intravenous anaesthetic developed by Organon in the 1990s as a companion candidate to the earlier compound Org 20599. It belongs to a series of 2-substituted (C2-morpholinyl) pregnane steroids engineered to combine the favourable receptor pharmacology of neuroactive steroids with the aqueous solubility needed for a practical injectable formulation, acting principally as a positive allosteric modulator (an agent that amplifies a receptor's response without being the primary trigger) of the GABA-A receptor (the brain's main inhibitory chloride ion channel). In computer-controlled infusion studies in healthy male volunteers the compound produced dose-related sedation and reversible loss of consciousness, but it was accompanied by prominent involuntary excitatory movements, injection-site venous pain, and slow equilibration with the effect site, and its clinical development was subsequently abandoned. It survives in the literature as a historical, niche illustration of the difficulty of translating neurosteroid GABA-A pharmacology into a usable anaesthetic.

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