Synonym
S 9871; S-9871; S9871; RX 801080; RX801080; RX-801080
IUPAC/Chemical Name
1H-Imidazole, 2-(2,3-dihydro-2-benzofuranyl)-4,5-dihydro-, (+-)-
InChi Key
LNWJIGHZWAERHO-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H12N2O/c1-2-4-9-8(3-1)7-10(14-9)11-12-5-6-13-11/h1-4,10H,5-7H2,(H,12,13)
SMILES Code
C1(C2OC3=CC=CC=C3C2)=NCCN1
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
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
188.23
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: Pauwels PJ, Rauly I, Wurch T. Dissimilar pharmacological responses by a new series of imidazoline derivatives at precoupled and ligand-activated alpha 2A-adrenoceptor states: evidence for effector pathway-dependent differential antagonism. J Pharmacol Exp Ther. 2003 Jun;305(3):1015-23. Epub 2003 Mar 20. PubMed PMID: 12649300.
2: Ball AJ, Flatt PR, McClenaghan NH. Stimulation of insulin secretion in clonal BRIN-BD11 cells by the imidazoline derivatives KU14r and RX801080. Pharmacol Res. 2000 Dec;42(6):575-9. PubMed PMID: 11058411.
3: Chan SL, Atlas D, James RF, Morgan NG. The effect of the putative endogenous imidazoline receptor ligand, clonidine-displacing substance, on insulin secretion from rat and human islets of Langerhans. Br J Pharmacol. 1997 Mar;120(5):926-32. PubMed PMID: 9138700; PubMed Central PMCID: PMC1564530.
4: Morgan NG, Chan SL, Brown CA, Tsoli E. Characterization of the imidazoline binding site involved in regulation of insulin secretion. Ann N Y Acad Sci. 1995 Jul 12;763:361-73. Review. PubMed PMID: 7677348.
5: Brown CA, Chan SL, Stillings MR, Smith SA, Morgan NG. Antagonism of the stimulatory effects of efaroxan and glibenclamide in rat pancreatic islets by the imidazoline, RX801080. Br J Pharmacol. 1993 Nov;110(3):1017-22. PubMed PMID: 7905338; PubMed Central PMCID: PMC2175820.
6: Joly G, Mouillé P, Schmitt H. Antagonistic effects of S9871 or (imidazolinyl-2)-2-dihydro 2,3 benzofurane and its stereoisomers on some central and peripheral actions of alpha 2-agonists. Arch Int Pharmacodyn Ther. 1985 Oct;277(2):180-91. PubMed PMID: 2865936.
7: Dabiré H, Mouillé P, Joly G, Schmitt H. Stereoselectivity of central alpha-adrenoceptors involved in sleep induced by clonidine in chickens. Neuropharmacology. 1985 Aug;24(8):709-12. PubMed PMID: 2875413.
8: Joly G, Mouillé P, Schmitt H. [Partial agonist properties of a new derivative of dihydrobenzofuran, S 9871, and its stereoisomers in pithed rats]. C R Seances Soc Biol Fil. 1985;179(1):70-3. French. PubMed PMID: 2862976.
9: Joly G, Mouillé P, Dabiré H, Lucet B, Schmitt H. Pre- and postsynaptic alpha-adrenoceptor blocking properties of a new dihydrobenzofurane derivative (imidazolinyl-2)-2-dihydro 2,3 benzofurane (S 9871) and its stereoisomers in rats. Arch Int Pharmacodyn Ther. 1984 Jun;269(2):277-86. PubMed PMID: 6148045.
10: Joly G, Mouillé P, Dabiré H, Schmitt H. [Effect of 2 new derivatives of imidazoline and their optical isomers on postsynaptic alpha adrenergic receptors in pithed rats]. C R Acad Sci III. 1984;299(4):73-5. French. PubMed PMID: 6149800.
