Synonym
Flutoprazepam; Restar; Restas; Flutoprazepamum;
IUPAC/Chemical Name
2H-1,4-Benzodiazepin-2-one, 7-chloro-1-(cyclopropylmethyl)-5-(o-fluorophenyl)-1,3-dihydro-
InChi Key
OFVXPDXXVSGEPX-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H16ClFN2O/c20-13-7-8-17-15(9-13)19(14-3-1-2-4-16(14)21)22-10-18(24)23(17)11-12-5-6-12/h1-4,7-9,12H,5-6,10-11H2
SMILES Code
O=C1N(CC2CC2)C3=CC=C(Cl)C=C3C(C4=CC=CC=C4F)=NC1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
342.80
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Conti I, Sarati S, Caccia S. Propranolol does not alter flutoprazepam kinetics and metabolism in the rat. Eur J Drug Metab Pharmacokinet. 1991 Jan-Mar;16(1):53-8. PubMed PMID: 1936062.
2: Barzaghi N, Leone L, Monteleone M, Tomasini G, Perucca E. Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects. Eur J Drug Metab Pharmacokinet. 1989 Oct-Dec;14(4):293-8. PubMed PMID: 2633923.
3: Oki K, Sukamoto T, Ito K, Nose T. In vitro and ex vivo inhibition by flutoprazepam of [3H]flunitrazepam binding to mouse brain receptors. Arch Int Pharmacodyn Ther. 1984 Jun;269(2):180-6. PubMed PMID: 6148044.
4: Moser L, Macciocchi A, Plum H, Bückmann. Effect of flutoprazepam on skills essential for driving motor vehicles. Arzneimittelforschung. 1990 May;40(5):533-5. PubMed PMID: 1974429.
5: Kozaki A, Sakurai S, Awata N. [Metabolic fate of flutoprazepam (KB-509). IV. Pharmacokinetics of flutoprazepam-2-14C and desalkylflutoprazepam-2-14C in dog plasma]. Yakugaku Zasshi. 1982 Dec;102(12):1177-83. Japanese. PubMed PMID: 7182452.
6: Richards BL, Whittle SL, Buchbinder R. Muscle relaxants for pain management in rheumatoid arthritis. Cochrane Database Syst Rev. 2012 Jan 18;1:CD008922. doi: 10.1002/14651858.CD008922.pub2. Review. PubMed PMID: 22258993.
7: Ueki S, Sukamoto T, Watanabe S, Yamamoto T, Kataoka Y, Shibata S, Suwandi D, Shibata K, Takano M, Sato Y. [Behavioral effects of flutoprazepam (KB-509) and its metabolites]. Nihon Yakurigaku Zasshi. 1982 Jul;80(1):15-30. Japanese. PubMed PMID: 6890927.
8: Fukinaga M, Ishizawa K, Kamei C. Anticonvulsant properties of 1,4-benzodiazepine derivatives in amygdaloid-kindled seizures and their chemical structure-related anticonvulsant action. Pharmacology. 1998 Nov;57(5):233-41. PubMed PMID: 9742288.
9: Sukamoto T, Aikawa K, Itoh K, Nose T. [Psycopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509) (author's transl)]. Nihon Yakurigaku Zasshi. 1980 Sep;76(6):447-68. Japanese. PubMed PMID: 7203280.
10: Fukuda T, Itoh K, Nose T. [Antiulcerogenic action of 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin- 2-one (KB-509), a new benzodiazepine derivative]. Nihon Yakurigaku Zasshi. 1981 Mar;77(3):273-80. Japanese. PubMed PMID: 7052359.
