Related CAS #
139751-07-8 (citrate); 110588-56-2 (free base); 111922-05-5 (maleate)
Synonym
Noberastine; R 64947; R-64947; R64947;
IUPAC/Chemical Name
3-((5-methylfuran-2-yl)methyl)-N-(piperidin-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine
InChi Key
VNIOQSAWKLOGLY-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H21N5O/c1-12-4-5-14(23-12)11-22-16-15(3-2-8-19-16)21-17(22)20-13-6-9-18-10-7-13/h2-5,8,13,18H,6-7,9-11H2,1H3,(H,20,21)
SMILES Code
CC1=CC=C(CN2C(NC3CCNCC3)=NC4=CC=CN=C42)O1
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
311.38
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: Wood-Baker R, Emanuel MB, Hutchinson K, Howarth PH. The time course of action of three differing doses of noberastine, a novel H1-receptor antagonist, on histamine-induced skin wheals and the relationship to plasma drug concentrations in normal human volunteers. Br J Clin Pharmacol. 1993 Feb;35(2):166-70. PubMed PMID: 8095149; PubMed Central PMCID: PMC1381509.
2: Kamali F, Emanuel M, Rawlins MD. A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. Eur J Clin Pharmacol. 1991;40(1):83-5. PubMed PMID: 1676366.
3: Knight A, Drouin MA, Yang WH, Alexander M, Del Carpio J, Arnott WS. Clinical evaluation of the efficacy and safety of noberastine, a new H1 antagonist, in seasonal allergic rhinitis: a placebo-controlled, dose-response study. J Allergy Clin Immunol. 1991 Dec;88(6):926-34. PubMed PMID: 1683882.
4: Lau HY, Tsang CW, Wong PP. Effects of acrivastine, azelastine, cetirizine and noberastine on rat peritoneal mast cells. Inflamm Res. 1995 Apr;44 Suppl 1:S30-1. PubMed PMID: 8520987.
5: Desager JP, Horsmans Y. Pharmacokinetic-pharmacodynamic relationships of H1-antihistamines. Clin Pharmacokinet. 1995 May;28(5):419-32. Review. PubMed PMID: 7614779.
6: Rodríguez Paredes A, González JL. [Data on the safety of antihistaminics obtained from published clinical trials]. Allergol Immunopathol (Madr). 2000 Sep-Oct;28(5):272-7. Review. Spanish. PubMed PMID: 11270088.