A 943931 dihydrochloride
Discontinued Product
Chemical Name: 4-((3R)-3-amino-pyrrolidin-1-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-ylamine
Purity: ≥98%
Biological Activity
A 943931 dihydrochloride is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Cowart et al.
J.Med.Chem., 2008;51:6547 -
Histamine H4-Receptors Inhibit Mast Cell Renin Release in Ischemia/Reperfusion via PKC{epsilon}-Dependent Aldehyde Dehydrogenase Type-2 Activation.
Aldi et al.
J.Pharmacol.Exp.Ther., 2014;349:508 -
Molecular and biochemical pharmacology of the histamine H4 receptor.
Leurs et al.
Br.J.Pharmacol., 2009;157:14
Product Datasheets
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Citations for A 943931 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for A 943931 dihydrochloride include:
2 Citations: Showing 1 - 2
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Dopaminergic regulation of vestibulo-cerebellar circuits through unipolar brush cells.
Authors: Yevgenia Et al.
Elife 2022;11
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Mast Cells in the Developing Brain Determine Adult Sexual Behavior.
Authors: Lenz Et al.
J Neurosci 2018;38:8044
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