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MedKoo Cat#: 414447 | Name: Noberastine citrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Noberastine citrate, a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.

Chemical Structure

Noberastine citrate
Noberastine citrate
CAS#139751-07-8 (citrate)

Theoretical Analysis

MedKoo Cat#: 414447

Name: Noberastine citrate

CAS#: 139751-07-8 (citrate)

Chemical Formula: C23H29N5O8

Exact Mass: 503.2016

Molecular Weight: 503.51

Elemental Analysis: C, 54.87; H, 5.81; N, 13.91; O, 25.42

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
139751-07-8 (citrate); 110588-56-2 (free base); 111922-05-5 (maleate)
Synonym
Noberastine citrate; R83546; R 83546; R-83546
IUPAC/Chemical Name
3-((5-methylfuran-2-yl)methyl)-N-(piperidin-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine 2-hydroxypropane-1,2,3-tricarboxylate
InChi Key
VXIJMTRTCJNTMW-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H21N5O.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h2-5,8,13,18H,6-7,9-11H2,1H3,(H,20,21);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
SMILES Code
Cc1ccc(Cn(c(NC2CCNCC2)n3)c4c3cccn4)o1.OC(CC(CC(O)=O)(C(O)=O)O)=O
Appearance
Solid powder
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 503.51 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.

Recalculate based on batch purity %
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.