GT 2016 - CAS 152241-24-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Histamine Receptor
GT 2016 is a high affinity and brain-penetrant histamine H3 receptor antagonist (Ki = 43.8 nM). It displays selectivity against H1 and H2 receptors (IC50 >10 μM). GT 2016 increases the release of histamine in the cerebral cortex. GT 2016 exhibits no effect on histamine methyltransferase in vitro at concentrations up to 3 μM.
Brife Description:
histamine H3 receptor antagonist
≥98% by HPLC
Canonical SMILES:
1.Histaminergic ligands attenuate barrel rotation in rats following unilateral labyrinthectomy.
Pan JB;O'Neill AB;Hancock AA;Sullivan JP;Brioni JD Methods Find Exp Clin Pharmacol. 1998 Nov;20(9):771-7.
In this paper we present a unilateral labyrinthectomy (UL) surgical procedure in rats that was derived from previous techniques. The utility of this model to assess vestibular dysfunction was evaluated by examining the ability of clinically used histaminergic agents and more selective H3 receptor antagonists to attenuate of UL-induced body rotations. Unilateral labyrinthectomy was performed by injection of ethanol into the rat right inner ear. An elevated body rotation test (EBRT) was used to assess the abnormal rotational behavior induced by UL. Scores of "3" to "0" were used to characterize the degree of abnormal behavior according to the latency of body rotations to begin. Our results demonstrate that: i) 100 microliters ethanol induced robust behavioral changes, which was used in further experiments; ii) the clinically used antivertigo agent, astemizole, significantly reduced the rotational behavior in UL rats; iii) the more potent H3 antagonists, thioperamide and GT-2016, were more efficacious than betahistine, a mixed H3 antagonist and H1 agonist. These results indicate that this model may be a potential tool for testing novel drugs for antivertigo effects and provide better support to the role of the histaminergic system in the control of vestibular function.
2.Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies.
Tedford CE;Yates SL;Pawlowski GP;Nalwalk JW;Hough LB;Khan MA;Phillips JG;Durant GJ;Frederickson RC J Pharmacol Exp Ther. 1995 Nov;275(2):598-604.
GT-2016, a non-thiourea-containing imidazole, has been developed as a histamine H3 antagonist. In vitro and in vivo studies in rats were conducted to characterize receptor selectivity and autoreceptor functionality for GT-2016. GT-2016 demonstrated high affinity (43.8 +/- 3.0 nM) and selectivity for the histamine H3 receptor in vitro. In vivo, GT-2016 (3, 10 and 30 mg/kg i.p. and p.o.) was shown to cross the blood-brain barrier and dose-dependently bind to cortical histamine H3 receptors. GT-2016 induced dose-dependent increases in histamine turnover at concentrations that exhibited significant histamine H3 receptor occupancy. Also, in vivo microdialysis experiments were conducted in awake, freely moving rats treated with GT-2016. GT-2016 (10 and 30 mg/kg i.p.) increased histamine release by approximately 75% above baseline within 1 hr, and elevated histamine release was observed for up to 2.5 hr after the higher dose. In contrast, GT-2016 was devoid of activity on histamine methyltransferase in vitro at concentrations up to 3 microM. Taken together, the results show that GT-2016 crosses the blood-brain barrier, binds to H3 receptors and increases the release of histamine in the cerebral cortex, consistent with blockade of presynaptic H3 autoreceptors.
3.Pharmacological evaluation of an in vivo model of vestibular dysfunction in the rat.
O'Neill AB;Pan JB;Sullivan JP;Brioni JD Methods Find Exp Clin Pharmacol. 1999 May;21(4):285-9.
A unilateral microinjection of either histamine or kainic acid was made into the medial vestibular nucleus of rats, eliciting robust barrel rotations that were evaluated by an elevated body-rotation test. Systemic pretreatment with betahistine or GT-2016 significantly attenuated the kainic acid-induced barrel rotations. These data indicate that the animal model described herein may represent a new model to identify novel drugs with potential antivertigo properties.
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CAS 152241-24-2 GT 2016

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