GT 2016

Discontinued Product

2419 has been discontinued.

View all Histamine H<sub>3</sub> Receptors products.
Description: Selective H3 antagonist
Chemical Name: 5-Cyclohexyl-1-[4-(1H-imidazol-5-yl)-1-piperidinyl]-1-pentanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for GT 2016

GT 2016 is a 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 for GT 2016

M. Wt 317.47
Formula C19H31N3O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 152241-24-2
PubChem ID 9839975
InChI Key YTCGNPGLMAECND-UHFFFAOYSA-N
Smiles O=C(CCCCC3CCCCC3)N(CC2)CCC2C1=CN=CN1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for GT 2016

References are publications that support the biological activity of the product.

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

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Keywords: GT 2016, GT 2016 supplier, GT2016, histamine, h3, antagonists, histaminergic, selective, brain, penetrant, centrally, active, Histamine, H3, Receptors, 2419, Tocris Bioscience

Citations for GT 2016

Citations are publications that use Tocris products.

Currently there are no citations for GT 2016.

Reviews for GT 2016

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.

Alzheimer's Disease Poster

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.