Synonym
L 663581; L-663581; L663581; FG-8205; FG 8205; FG8205;
IUPAC/Chemical Name
7-chloro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-4,5-dihydro-6H-benzo[f]imidazo[1,5-a][1,4]diazepin-6-one
InChi Key
SEWXZWMBVGJJPG-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H16ClN5O2/c1-9(2)16-20-15(21-25-16)14-12-7-22(3)17(24)13-10(18)5-4-6-11(13)23(12)8-19-14/h4-6,8-9H,7H2,1-3H3
SMILES Code
O=C1N(C)CC2=C(C3=NOC(C(C)C)=N3)N=CN2C4=CC=CC(Cl)=C14
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
357.79
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: Guscott MR, Cook GP, Bristow LJ. Contextual fear conditioning and baseline startle responses in the rat fear-potentiated startle test: a comparison of benzodiazepine/gamma-aminobutyric acid-A receptor agonists. Behav Pharmacol. 2000 Sep;11(6):495-504. PubMed PMID: 11103915.
2: Hadingham KL, Wafford KA, Thompson SA, Palmer KJ, Whiting PJ. Expression and pharmacology of human GABAA receptors containing gamma 3 subunits. Eur J Pharmacol. 1995 Nov 30;291(3):301-9. PubMed PMID: 8719414.
3: Jackson A. State-dependent effects of atypical benzodiazepine-receptor agonists. Psychopharmacology (Berl). 1995 Jun;119(4):399-404. PubMed PMID: 7480519.
4: Lin JH, Chen IW, Lin TH. Blood-brain barrier permeability and in vivo activity of partial agonists of benzodiazepine receptor: a study of L-663,581 and its metabolites in rats. J Pharmacol Exp Ther. 1994 Dec;271(3):1197-202. PubMed PMID: 7996426.
5: Chen IW, Lin JH. Physiological disposition of L-663,581, a partial agonist of the benzodiazepine receptor, in laboratory animals. Drug Metab Dispos. 1994 Sep-Oct;22(5):693-9. PubMed PMID: 7835219.
6: Stanhope KJ, Roe S, Dawson G, Draper F, Jackson A. Effect of the benzodiazepine receptor agonist, zolpidem, on palatable fluid consumption in the rat. Psychopharmacology (Berl). 1993;111(2):185-9. PubMed PMID: 7870950.
7: Tricklebank MD, Honoré T, Iversen SD, Kemp JA, Knight AR, Marshall GR, Rupniak NM, Singh L, Tye S, Watjen F, et al. The pharmacological properties of the imidazobenzodiazepine, FG 8205, a novel partial agonist at the benzodiazepine receptor. Br J Pharmacol. 1990 Nov;101(3):753-61. PubMed PMID: 1963808; PubMed Central PMCID: PMC1917729.
8: Lin TH, Lin JH. Effects of protein binding and experimental disease states on brain uptake of benzodiazepines in rats. J Pharmacol Exp Ther. 1990 Apr;253(1):45-50. PubMed PMID: 1970363.