Ro48-8684: Difference between revisions

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{{Drugbox

| Watchedfields = changed

| verifiedrevid = ~~450848725~~

| verifiedrevid = 451550070

| IUPAC_name = 3-(5-dipropylaminomethyloxazol-2-yl)-8-fluoro-5-methyl-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one

| IUPAC_name = 3-(5-dipropylaminomethyloxazol-2-yl)-8-fluoro-5-methyl-5,6-dihydro-4''H''-imidazo[1,5-''a''][1,4]benzodiazepin-6-one

| image = Ro48-8684_structure.png

| ~~width~~ = ~~200~~

| image = Ro48-8684.svg

| width = 242

| tradename =

| legal_status =

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| metabolism =

| elimination_half-life =

| excretion =

| CAS_number = 179634-04-9

| PubChem = 9866317

| ChemSpiderID = 8042008

| DrugBank_Ref = {{drugbankcite|correct|drugbank}}

| C=22 | H=26 | F=1 | N=5 | O=2

| smiles = CCCN(CC1=CN=C(C2=C(CN(C(C3=C4C=CC(F)=C3)=O)C)N4C=N2)O1)CCC

| molecular_weight = 411.472

| StdInChI = 1S/C22H26FN5O2/c1-4-8-27(9-5-2)12-16-11-24-21(30-16)20-19-13-26(3)22(29)17-10-15(23)6-7-18(17)28(19)14-25-20/h6-7,10-11,14H,4-5,8-9,12-13H2,1-3H3

| smiles = CCCN(CCC)Cc(cn3)oc3-c2ncn-1c2CN(C)C(=O)c4cc(F)ccc-14

| StdInChIKey = YKKLHEHNUYCLQQ-UHFFFAOYSA-N

}}

'''Ro48-8684''' is a water-soluble [[benzodiazepine]] derivative developed by [[Hoffman-LaRoche]] in the 1990s, which was designed along with [[Ro48-6791]] as an improved replacement for [[midazolam]], but ultimately proved to have little advantages over the parent drug and has not been introduced into clinical practice.<ref>van Gerven JM, Roncari G, Schoemaker RC, Massarella J, Keesmaat P, Kooyman H, Heizmann P, Zell M, Cohen AF, Dingemanse J. Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. ''British Journal of Clinical Pharmacology~~''.~~ ~~1997~~ ~~Nov;~~44(5~~):487-93.~~ ~~PMID~~ 9384466</ref><ref>Albrecht S, Hering W, Ihmsen H, Schwilden H, Schüttler J. Pharmacokinetic-pharmacodynamic modeling in phase II of drug development. A comparative study with young and old volunteers with benzdiazepine as an example. ~~(German)~~ ~~''Anasthesiologie~~, Intensivmedizin, Notfallmedizin, Schmerztherapie~~''.~~ ~~1999~~ ~~Oct;~~34(10~~):634-7.~~ ~~PMID~~ 10548960</ref>

'''Ro48-8684''' is a water-soluble [[benzodiazepine]] derivative developed by [[Hoffman-LaRoche]] in the 1990s, which was designed along with [[Ro48-6791]] as an improved replacement for [[midazolam]], but ultimately proved to have little advantages over the parent drug and has not been introduced into clinical practice.<ref>{{cite journal | vauthors = van Gerven JM, Roncari G, Schoemaker RC, Massarella J, Keesmaat P, Kooyman H, Heizmann P, Zell M, Cohen AF, Dingemanse J | display-authors = 6 | title = Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects | journal = British Journal of Clinical Pharmacology | volume = 44 | issue = 5 | pages = 487–93 | date = November 1997 | pmid = 9384466 | pmc = 2042863 | doi = 10.1046/j.1365-2125.1997.t01-1-00613.x }}</ref><ref>{{cite journal | vauthors = Albrecht S, Hering W, Ihmsen H, Schwilden H, Schüttler J | title = [Pharmacokinetic-pharmacodynamic modeling in phase II of drug development. A comparative study with young and old volunteers with benzdiazepine as an example] | journal = Anästhesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie | volume = 34 | issue = 10 | pages = 634–7 | date = October 1999 | pmid = 10548960 | doi = 10.1055/s-1999-213 }}</ref>

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== See also ==

⚫

==See also==

*[[Benzodiazepine]]

==References==

== References ==

[[Category:~~Benzodiazepines~~]]

[[Category:Abandoned drugs]]

[[Category:~~Oxazoles~~]]

[[Category:GABAA receptor positive allosteric modulators]]

[[Category:Drugs developed by Hoffmann-La Roche]]

[[Category:Imidazobenzodiazepines]]

[[Category:Lactams]]

[[Category:~~Organofluorides~~]]

[[Category:Fluoroarenes]]

[[Category:~~Hoffmann-La Roche~~]]

[[Category:Oxazoles]]