CP 99994 dihydrochloride
High affinity NK1 antagonist (Ki = 0.145 nM in vitro). Also displays high ex vivo binding potency in gerbil striatum (IC50 = 36.8 nM). Attenuates endothelium-dependent contraction induced by substance P.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Desiccate at RT|
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 369.33. 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||2.71 mL||13.54 mL||27.08 mL|
|5 mM||0.54 mL||2.71 mL||5.42 mL|
|10 mM||0.27 mL||1.35 mL||2.71 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Shirahase et al (1995) Endothelium-dependent contraction in intrapulmonary arteries: mediation by endothelial NK1 receptors and TXA2. Br.J.Pharmacol. 115 1215 PMID: 7582548
Duffy et al (2002) Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. J.Pharmacol.Exp.Ther. 301 536 PMID: 11961054
Lindstrom et al (2007) Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy. J.Pharmacol.Exp.Ther. 322 1286 PMID: 17575073
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1 Citation for CP 99994 dihydrochloride
Citations are publications that use Tocris products. Selected citations for CP 99994 dihydrochloride include:
Horn et al (2013) Novel dynamic measures of emetic behavior in musk shrews. Nature 179 60 PMID: 23953843
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.