(R)-(-)-alpha-Methylhistamine dihydrobromide - CAS 868698-49-1
Category: Inhibitor
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Molecular Formula:
C6H11N3.2HBr
Molecular Weight:
287
COA:
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Targets:
Histamine Receptor
Description:
(R)-(-)-alpha-Methylhistamine dihydrobromide is a potent and high affinity histamine H3 agonist (KD = 50.3 nM) displaying > 200-fold selectivity over H4 receptors. It inhibits H3-mediated histamine synthesis and release in the CNS at nanomolar concentrations, and induces H4-mediated eosinophil shape change (EC50 = 66 nM).
Brife Description:
histamine H3 agonist
Purity:
≥99% by HPLC
Synonyms:
(R)-(-)-α-Methyl-1H-imidazole-4-ethanamine dihydrobromide
MSDS:
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InChIKey:
RWHNAAABSGVRDT-ZJIMSODOSA-N
InChI:
InChI=1S/C6H11N3.2BrH/c1-5(7)2-6-3-8-4-9-6;;/h3-5H,2,7H2,1H3,(H,8,9);2*1H/t5-;;/m1../s1
Canonical SMILES:
CC(CC1=CN=CN1)N.Br.Br
1.Studies on the pharmacology of the novel histamine H3 receptor agonist Sch 50971.
Hey JA;Aslanian R;Bolser DC;Chapman RW;Egan RW;Rizzo CA;Shih NY;Fernandez X;McLeod RL;West R;Kreutner W Arzneimittelforschung. 1998 Sep;48(9):881-8.
Experiments were performed to characterize the pharmacology of Sch 50971 ((+)-trans-4-(4(R)-methyl-3(R)-pyrolidinyl)-1H-imidazole dihydrochloride, CAS 167610-28-8), a novel histamine H3 receptor agonist. The activity of Sch 50971 was compared with that of (R)-alpha-methylhistamine (CAS 75614-87-8), a potent and moderately selective agonist of histamine H3 receptors, in a series of in vitro and in vivo assays. Sch 50971 is a high affinity, selective H3 receptor agonist in vitro and in vivo. Sch 50971 inhibits [3H]-N-alpha-methylhistamine (CAS 673-50-7) binding to the histamine H3 receptor in human brain (Ki = 5.0 nmol/l) and guinea pig brain (Ki = 2.5 nmol/l). Sch 50971 also inhibits electric field stimulated guinea pig ileum contractions (pD2 = 7.47) and decreases [3H]-norepinephrine (CAS 51-41-2) release (pD2 = 7.48) from guinea pig pulmonary artery by activation of presynaptic inhibitory H3 receptors. The in vitro effects of Sch 50971 are antagonized by low concentrations of a selective H3 antagonist, thioperamide (CAS 106243-16-7). Sch 50971 has low affinity (IC50's > 10 mumol/l) for histamine H1, dopamine D1 and D2, serotonin 5-HT2 and muscarinic cholinergic receptors. It also does not exhibit histamine H2-antagonist activity.
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CAS 868698-49-1 (R)-(-)-alpha-Methylhistamine dihydrobromide

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