Chemical Name: N-[(1R)-1-[(4-Chlorophenyl)methyl]-2-[4-cyclohexyl-4-(1H-1,2,4-trazol-1-ylmethyl)-1-piperidinyl]-2-oxoethyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide
Biological ActivityTHIQ is a potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 1.2, 761 and 2067 nM for human MC4, MC3 and MC1 receptors respectively). Enhances intracavernosal pressure and stimulates erectile activity in rats ex copula following systemic administration.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula.
Martin et al.
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ".
Mutulis et al.
Design and pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-methyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective melanocorti
Sebhat et al.
Citations for THIQ
The citations listed below are publications that use Tocris products. Selected citations for THIQ include:
3 Citations: Showing 1 - 3
A neural basis for melanocortin-4 receptor-regulated appetite.
Authors: Garfield Et al.
Nat Neurosci 2015;18:863
A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retained melanocortin-4 receptor mutants.
Authors: Huang and Tao
Front Pharmacol 2014;10:817
Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons.
Authors: Sohn Et al.
Int J Biol Sci 2013;152:612
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Recently, we demonstrated that the deletion of the NFKB1 gene, which encodes the p50 NF-kappa B subunit, causes impairment in social behaviours, with reductions in social interactions in mice. In this work, we tested the acute effects of THIQ, a selective melanocortin 4 receptor (MC4R) agonist. THIQ treatment increased social interactions both in wild type and p50-/- mice. In particular, after treatment with THIQ, p50-/- mice showed a prosocial behaviour analogous to that of basal WT mice.