Posovolone
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| Other names | CO-134444; Co 134444; V-134444; 3β-Hydroxy-21-(1H-imidazol-1-yl)-3α-(methoxymethyl)-5α-pregnan-20-one |
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| Chemical and physical data | |
| Formula | C26H40N2O3 |
| Molar mass | 428.617 g·mol−1 |
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Posovolone (developmental code name Co 134444) is a synthetic neurosteroid which was under development as a sedative/hypnotic medication for the treatment of insomnia.[1][2] [3][4] It is orally active and acts as a GABAA receptor positive allosteric modulator.[1][5][2] In animals, posovolone shows anticonvulsant, anxiolytic-like, ataxic, and sleep-promoting effects and appeared to produce effects similar to those of pregnanolone.[2][6] Development of the agent was started by 1999 and appears to have been discontinued by 2007.[1][6] In 2021, an INN was registered for posovolone with the descriptor of "antidepressant".[5] Posovolone was originally developed by Purdue Pharma.[1]
See also
[edit]References
[edit]- ^ a b c d "CO 134444 - AdisInsight".
- ^ a b c Vanover KE, Hogenkamp DJ, Lan NC, Gee KW, Carter RB (May 2001). "Behavioral characterization of Co 134444 (3alpha-hydroxy-21-(1'-imidazolyl)-3beta-methoxymethyl-5alpha- pregnan-20-one), a novel sedative-hypnotic neuroactive steroid". Psychopharmacology (Berl). 155 (3): 285–91. doi:10.1007/s002130100695. PMID 11432691. S2CID 44353086.
- ^ Hamilton NM (August 2002). "Interaction of steroids with the GABA(A) receptor". Curr Top Med Chem. 2 (8): 887–902. doi:10.2174/1568026023393570. PMID 12171578.
- ^ Belelli D, Hogenkamp D, Gee KW, Lambert JJ (May 2020). "Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor". Neurobiol Stress. 12: 100207. doi:10.1016/j.ynstr.2019.100207. PMC 7231973. PMID 32435660.
- ^ a b https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl126.pdf#page=137 [bare URL PDF]
- ^ a b Vanover KE, Edgar DM, Seidel WF, Hogenkamp DJ, Fick DB, Lan NC, Gee KW, Carter RB (December 1999). "Response-rate suppression in operant paradigm as predictor of soporific potency in rats and identification of three novel sedative-hypnotic neuroactive steroids". J Pharmacol Exp Ther. 291 (3): 1317–23. PMID 10565857.
External links
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