Cat. No. 2419
Chemical Name: 5-Cyclohexyl-1-[4-(1H-imidazol-5-yl
Biological ActivityHigh 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Tedford et al (1999) Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1160. PMID: 10215700.
Yates et al (1999) Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1151. PMID: 10215699.
Tedford et al (1995) Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. J.Pharmacol.Exp.Ther. 275 598. PMID: 7473144.
If you know of a relevant reference for GT 2016 please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses GT 2016 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: GT 2016, supplier, GT2016, histamine, h3, antagonists, histaminergic, selective, brain, penetrant, centrally, active, Tocris Bioscience, Histamine H3 Receptor Antagonist products
Find multiple products by catalog number
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.