Synonym
Flumezapine; LY 120363; LY120363
IUPAC/Chemical Name
10H-Thieno(2,3-b)(1,5)benzodiazepine, 7-fluoro-2-methyl-4-(4-methyl-1-piperazinyl)-
InChi Key
JBHUBOISLBWHAR-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H19FN4S/c1-11-9-13-16(22-7-5-21(2)6-8-22)19-15-10-12(18)3-4-14(15)20-17(13)23-11/h3-4,9-10,20H,5-8H2,1-2H3
SMILES Code
CN1CCN(C2=NC3=CC(F)=CC=C3NC4=C2C=C(C)S4)CC1
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
>3 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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
330.43
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: Fuller RW, Mason NR. Flumezapine, an antagonist of central dopamine and serotonin receptors. Res Commun Chem Pathol Pharmacol. 1986 Oct;54(1):23-34. PubMed PMID: 2879325.
2: Fuller RW, Snoddy HD. Flumezapine and zotepine: 5-hydroxytryptamine antagonism not involved in the lack of synergism of these antipsychotic drugs with amfonelic acid in rats. J Pharm Pharmacol. 1985 Oct;37(10):755-6. PubMed PMID: 2867152.
3: Sullivan HR, Franklin RB. In vitro thiomethylation. Studies with flumezapine. Drug Metab Dispos. 1985 May-Jun;13(3):276-8. PubMed PMID: 2861982.
4: Fuller RW, Snoddy HD. Central dopamine receptors mediating pergolide-induced elevation of serum corticosterone in rats. Characterization by the use of antagonists. Neuropharmacology. 1984 Dec;23(12A):1389-94. PubMed PMID: 6527743.
5: Chakrabarti JK, Hotten TM, Pullar IA, Type NC. Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. J Med Chem. 1989 Dec;32(12):2573-82. PubMed PMID: 2573732.
6: Altar CA, Boyar WC, Wasley A, Gerhardt SC, Liebman JM, Wood PL. Dopamine neurochemical profile of atypical antipsychotics resembles that of D-1 antagonists. Naunyn Schmiedebergs Arch Pharmacol. 1988 Aug;338(2):162-8. PubMed PMID: 2903451.
7: Estall LB, Cooper SJ. Differential effects of benzodiazepine receptor ligands on isotonic saline and water consumption in water-deprived rats. Pharmacol Biochem Behav. 1987 Feb;26(2):247-52. PubMed PMID: 3033695.
