A 943931 dihydrochloride

Discontinued Product

A 943931 dihydrochloride (Cat. No. 3753) has been withdrawn from sale for commercial reasons.
Description: Potent and selective H4 antagonist
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% (HPLC)
Citations (1)
Literature (2)

Biological Activity for A 943931 dihydrochloride

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 for A 943931 dihydrochloride

M. Wt 368.31
Formula C17H21N5.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1227675-50-4
PubChem ID 56972240
Smiles NC1=NC(N4C[C@H](N)CC4)=C2C(C(C=CC=C3)=C3CCC2)=N1.Cl.Cl

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.

Product Datasheets for A 943931 dihydrochloride

References for A 943931 dihydrochloride

References are publications that support the biological activity of the product.

Cowart et al (2008) 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. J.Med.Chem. 51 6547 PMID: 18817367

Leurs et al (2009) Molecular and biochemical pharmacology of the histamine H4 receptor. Br.J.Pharmacol. 157 14 PMID: 19413568

Aldi et al (2014) Histamine H4-Receptors Inhibit Mast Cell Renin Release in Ischemia/Reperfusion via PKC{epsilon}-Dependent Aldehyde Dehydrogenase Type-2 Activation. J.Pharmacol.Exp.Ther. 349 508 PMID: 24696042

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Keywords: A 943931 dihydrochloride, A 943931 dihydrochloride supplier, A943931, potent, selective, H4, histamine, 4, antagonists, histaminergics, receptors, Histamine, Receptors, 3753, Tocris Bioscience

1 Citation for A 943931 dihydrochloride

Citations are publications that use Tocris products. Selected citations for A 943931 dihydrochloride include:

Lenz et al (2018) Mast Cells in the Developing Brain Determine Adult Sexual Behavior. J Neurosci 38 8044 PMID: 30093566

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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GPCR Product Listing

GPCR Product Listing

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Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.