A 987306 - CAS 1082954-71-9
Category: Inhibitor
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Molecular Formula:
C18H25N5O
Molecular Weight:
327.42
COA:
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Targets:
Histamine Receptor
Description:
A 987306 is a potent histamine H4 receptor antagonist (pKi = 8.24 and 8.47 in human and rat H4 receptors, respectively) with 162-, 620-, and > 1600-fold selectivity over human H3, H1 and H2 receptors. It suppresses zymosan-induced neutrophil reflux and attenuates thermal hypersensitivity in vivo (ED50 = 42 μmol/kg, ip).
Brife Description:
histamine H4 receptor antagonist
Purity:
≥98% by HPLC
Synonyms:
(±)-(7aR,11aR)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
MSDS:
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InChIKey:
DJKJVWJQAVGLHJ-WCQYABFASA-N
InChI:
InChI=1S/C18H25N5O/c19-18-21-16-12(17(22-18)23-9-7-20-8-10-23)5-6-14-15(16)11-3-1-2-4-13(11)24-14/h11,13,20H,1-10H2,(H2,19,21,22)/t11-,13+/m0/s1
Canonical SMILES:
C1CCC2C(C1)C3=C(O2)CCC4=C3N=C(N=C4N5CCNCC5)N
1.Azines as histamine H4 receptor antagonists.
Lazewska D;Kiec-Kononowicz K Front Biosci (Schol Ed). 2012 Jan 1;4:967-87.
Since 2000, when the histamine H4 receptor (H4R) was cloned, it has constituted an interesting target for drug development. Pharmacological studies suggest the potential utility of histamine H4R antagonists/inverse agonists in the treatment of inflammatory diseases, e.g. allergic rhinitis, asthma, atopic dermatitis, colitis, or pruritus. The first H4R ligands were non-selective compounds, but intensive chemical and pharmacological work has led to the discovery of highly potent and selective H4R antagonists (e.g. JNJ7777120, CZC-13788, PF-2988403, A-940894, A-987306). The first compound (UR-63325) has finally entered into clinical studies for the treatment of allergic respiratory diseases (completing the phase I ascending dose trial) and has been found to be safe and well tolerated. The number of scientific publications and patent applications in the H4 field is increasing annually. Among the diverse chemical structures of the H4R antagonists described a 2-aminopyrimidine scaffold is repeatedly found. This review looked at recent advances in the search for H4R antagonists as reflected in patent applications/patents and peer-reviewed publications over the last two years. The work concerns azines (mono-, di-, triazines) and their fused analogues.
2.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Liu H;Altenbach RJ;Carr TL;Chandran P;Hsieh GC;Lewis LG;Manelli AM;Milicic I;Marsh KC;Miller TR;Strakhova MI;Vortherms TA;Wakefield BD;Wetter JM;Witte DG;Honore P;Esbenshade TA;Brioni JD;Cowart MD J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618.
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine, 4 (A-987306) is a new histamine H(4) antagonist. The compound is potent in H(4) receptor binding assays (rat H(4), K(i) = 3.4 nM, human H(4) K(i) = 5.8 nM) and demonstrated potent functional antagonism in vitro at human, rat, and mouse H(4) receptors in cell-based FLIPR assays. Compound 4 also demonstrated H(4) antagonism in vivo in mice, blocking H(4)-agonist induced scratch responses, and showed anti-inflammatory activity in mice in a peritonitis model. Most interesting was the high potency and efficacy of this compound in blocking pain responses, where it showed an ED(50) of 42 mumol/kg (ip) in a rat post-carrageenan thermal hyperalgesia model of inflammatory pain.
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CAS 1082954-71-9 A 987306

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