Toggle Nav
Close
  • Menu
  • Setting

A 331440 dihydrochloride

Catalog No.
B7698
H3 receptor antagonist,non-imidazole,high affinity
Grouped product items
SizePriceStock Qty
10mg
$345.00
Please inquire
50mg
$1,430.00
Please inquire
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

A-331440 is described here instead of A-331440 dihydrochloride. A-331440 is an antagonist of non-imidazole histamine H3 receptor with an IC50 value of 22.7 nM for human cortex histamine H3 [1].

Histamine, as a neurotransmitter, is important in homeostasis and physiology. In the CNS, histamine released has the potential to interact with H1, H2, H3 and possibly H4 receptors. All the receptors are G-protein coupled receptors [2].

In HEK 293 cells stably transfected with rat or human histamine H3 receptors, A-331440 was tested for its ability to antagonize increasing calcium mobilization in response to (R)-α-methylhistamine and showed pKb ± S.E.M. values of 7.38 ± 0.10 and 7.37 ± 0.29 for rat histamine H3 and human histamine H3, respectively [1].

In mice, treatment with A-331440 at a dose of 100 mg/kg resulted in piloerection and hypoactivity in the first 2 h, but diminished thereafter. In naive male CD-1 mice, administration with comparable doses of A-331440 i.p. also produced similar data. By day 28, mice treated with A-331440 at the intermediate dose weighed 35.7 ± 0.93 g with an average weight loss of 5.3 ± 0.99 g. The high dose of A-331440 (15 mg/kg, p.o., b.i.d.) produced a marked and sustained weight loss [1].

References:
[1].  Hancock AA, Bennani YL, Bush EN, et al. Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. European journal of pharmacology, 2004, 487(1): 183-197.
[2].  Hancock AA, Diehl MS, Faghih R, et al. In vitro Optimization of Structure Activity Relationships of Analogues of A-331440 Combining Radioligand Receptor Binding Assays and Micronucleus Assays of Potential Antiobesity Histamine H3 Receptor Antagonists. Basic & clinical pharmacology & toxicology, 2004, 95(3): 144-152.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt422.39
Cas No.1049740-32-0
FormulaC22H27N3O·2HCl
Solubility<42.24mg/ml in H2O; <8.45mg/ml in DMSO
Chemical Name(R)-4'-(3-(3-(dimethylamino)pyrrolidin-1-yl)propoxy)-[1,1'-biphenyl]-4-carbonitrile dihydrochloride
SDFDownload SDF
Canonical SMILESCN([C@](C1)([H])CCN1CCCOC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)C.Cl.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

A 331440 dihydrochloride