Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.
Sold for research purposes under agreement from GlaxoSmithKline
(Modifications: Leu-7 = R-γ-lactam-Leu, Met-8 = C-terminal amide)
|Storage||Desiccate at -20°C|
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.
|Solubility||Soluble to 1 mg/ml in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 921.12. 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||1.09 mL||5.43 mL||10.86 mL|
|5 mM||0.22 mL||1.09 mL||2.17 mL|
|10 mM||0.11 mL||0.54 mL||1.09 mL|
|50 mM||0.02 mL||0.11 mL||0.22 mL|
References are publications that support the products' biological activity.
Chang et al (2000) Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J.Pharmacol.Exp.Ther. 294 147 PMID: 10871306
Chizh et al (1995) Endogenous modulation of excitatory amino acid responsiveness by tachykinin NK1 and NK2 receptors in the rat spinal cord. Br.J.Pharmacol. 115 1013 PMID: 7582497
Deal et al (1992) Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J.Med.Chem. 35 4195 PMID: 1331460
If you know of a relevant reference for GR 64349, please let us know.
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Keywords: GR 64349, supplier, Potent, selective, NK2, agonists, Tachykinin, Receptors, Neurokinin, GR64349, GlaxoSmithKline, GSK, NK2, Receptor, NK2, Receptor, Tocris Bioscience
3 Citations for GR 64349
Citations are publications that use Tocris products. Selected citations for GR 64349 include:
Navarro et al (2015) The integrated hypothalamic tachykinin-kisspeptin system as a central coordinator for reproduction. Sci Rep 156 627 PMID: 25422875
León et al (2016) Direct actions of kisspeptins on GnRH neurons permit attainment of fertility but are insufficient to fully preserve gonadotropic axis activity. Sci.Rep. 6 19206 PMID: 26755241
Ruiz-Pino et al (2015) Effects and interactions of tachykinins and dynorphin on FSH and LH secretion in developing and adult rats. Endocrinology 156 576 PMID: 25490143
Do you know of a great paper that uses GR 64349 from Tocris? If so please let us know.
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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.