GT 2016
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Description: Selective H3 antagonist
Chemical Name: 5-Cyclohexyl-1-[4-(1H-imidazol-5-yl)-1-piperidinyl]-1-pentanone
Purity: ≥98%
Biological Activity
High affinity H3 receptor antagonist (Ki = 43.8 nM). Displays selectivity against H1 and H2 receptors (IC50 >10 μM). Increases the release of histamine in the cerebral cortex. Displays no activity at histamine methyltransferase in vitro at concentrations up to 3 μM. Brain penetrant.Technical Data
M.Wt:
317.47
Formula:
C19H31N3O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
152241-24-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
-
Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies.
Tedford et al.
J.Pharmacol.Exp.Ther., 1995;275:598 -
Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands.
Tedford et al.
J.Pharmacol.Exp.Ther., 1999;289:1160 -
Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.
Yates et al.
J.Pharmacol.Exp.Ther., 1999;289:1151
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