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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 317.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.15 mL||15.75 mL||31.5 mL|
|5 mM||0.63 mL||3.15 mL||6.3 mL|
|10 mM||0.31 mL||1.57 mL||3.15 mL|
|50 mM||0.06 mL||0.31 mL||0.63 mL|
References are publications that support the products' biological activity.
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
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
If you know of a relevant reference for GT 2016, please let us know.
View Related Products by Product Action
Keywords: GT 2016, supplier, GT2016, histamine, h3, antagonists, histaminergic, selective, brain, penetrant, centrally, active, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience
Citations for GT 2016
Citations are publications that use Tocris products.
Currently there are no citations for GT 2016. Do you know of a great paper that uses GT 2016 from Tocris? If so please let us know.
Reviews for GT 2016
There are currently no reviews for this product. Be the first to review GT 2016 and earn rewards!
Have you used GT 2016?
Submit a review and receive an Amazon gift card.
$10US/$10CAN/€7/£6 gift card for a review without an image
$25US/$25CAN/€18/£15 gift card for a review with an image
*Offer only valid in the USA / Canada, UK and EuropeSubmit a Review
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.