SB-205,384
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| Systematic (IUPAC) name | |
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but-2-ynyl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[3,2-e]pyridine-3-carboxylate
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| Identifiers | |
| CAS Number | 160296-13-9  |
| PubChem | CID 197690 |
| ChemSpider | 171116 |
| Chemical data | |
| Formula | C17H18N2O3S |
| Molar mass | 330.401 g/mol |
| 3D model (Jmol) | Interactive image |
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SB-205,384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.
SB-205,384 is a GABAA positive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes.[1][2] It has a novel mechanism of action, prolonging the duration of GABA-mediated chloride flux but without increasing the intensity of the response, and this may give it an unusual pharmacological profile,[3] with tests showing that it alters the firing of some populations of neurons while leaving others unaffected.[4] Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes.[5][6]
References[edit]
- ^ Heidelberg LS; Warren JW; Fisher JL (2013). "SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 subunits". J. Pharmacol. Exp. Ther. 347 (1): 235–41. doi:10.1124/jpet.113.207324. PMID 23902941.
- ^ Meadows, HJ; Kumar, CS; Pritchett, DB; Blackburn, TP; Benham, CD (1998). "SB-205384: a GABAA receptor modulator with novel mechanism of action that shows subunit selectivity". British Journal of Pharmacology. 123 (6): 1253–9. doi:10.1038/sj.bjp.0701721. PMC 1565273
. PMID 9559912. - ^ Meadows, HJ; Harries, MH; Thompson, M; Benham, CD (1997). "Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum". British Journal of Pharmacology. 121 (7): 1334–8. doi:10.1038/sj.bjp.0701251. PMC 1564816. PMID 9257911.
- ^ Ing, T; Poulter, MO (2007). "Diversity of GABA(A) receptor synaptic currents on individual pyramidal cortical neurons". The European Journal of Neuroscience. 25 (3): 723–34. doi:10.1111/j.1460-9568.2007.05331.x. PMID 17313570.
- ^ Navarro, JF; Burón, E; Martín-López, M (2006). "Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice". Psicothema. 18 (1): 100–4. PMID 17296016.
- ^ Navarro, JF; Burón, E; Martín-López, M (2008). "Effects of SB-205384, a positive modulator of alpha3-subunit-containing GABA-A receptors, on isolation-induced aggression in male mice". Psicothema. 20 (1): 144–7. PMID 18206077.
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