TCS 1102
Chemical Name: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
Purity: ≥98%
Biological Activity
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour. Brain penetrant.Technical Data
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.
Additional Information
Background References
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The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking.
Khoo et al.
PLoS One, 2017;12:e0173967 -
Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure.
Winrow et al.
Neuropharmacology, 2010;58:185 -
Proline bis-amides as potent dual orexin receptor antagonists.
Bergman et al.
Bioorg.Med.Chem.Letts, 2008;18:1425
Product Datasheets
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Citations for TCS 1102
The citations listed below are publications that use Tocris products. Selected citations for TCS 1102 include:
7 Citations: Showing 1 - 7
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Circadian regulation of developmental synaptogenesis via the hypocretinergic system.
Authors: Yu Et al.
Nat Commun 2023;14:3195
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Orexin Modulation of VTA Dopamine Neuron Activity: Relevance to Schizophrenia.
Authors: Daniel J Et al.
Int J Neuropsychopharmacol 2021;24:344-353
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The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking.
Authors: Khoo Et al.
PLoS One 2017;
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Blocking of orexin receptors in the paraventricular nucleus of the thalamus has no effect on the expression of conditioned fear in rats.
Authors: Dong Et al.
Front Behav Neurosci 2015;9:161
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Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area.
Authors: Mavanji Et al.
Sleep 2015;38:1361
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Orexinergic activation of medullary premotor neurons modulates the adrenal sympathoexcitation to hypothalamic glucoprivation.
Authors: Korim Et al.
Diabetes 2014;63:1895
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Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
Authors: Putula Et al.
Br J Pharmacol 2014;171:5816
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