Uses
Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM). It less potently agonizes the NK1 receptor (EC50 = 35 μM) and is without effect on the NK2 receptor. Senktide is used to study the action of the NK3 receptor in cells and in animals.
Biological Activity
Senktide is a selective Neurokinin NK3 tachykinin receptor agonist. Neurokinins (tachykinins) are members of a family of at least three neuropeptides, substance P, neurokinin A, and neurokinin B (NKB), with each mediating their biological effects through binding to a preferred G-protein-coupled receptor termed NK1, NK2, or NK3, respectively. All three NK receptors are expressed in regions of the central nervous system th at are related to emotion and cognition (i.e., amygdala and hippocampus) and have been linked to various degrees in psychiatric disorders. Neurokinin receptors, including NK3 receptors, are also expressed in the motor and sensory systems of the digestive tract.', 'Senktide treatment in follicular phase goats enhances the liberation of luteinizing hormone (LH) and advance the time of ovulation. Senktide has the ability to suppress gonadotropin-releasing hormone (GnRH) transcription. Treatment with senktide stimulates c-Fos and improve activator protein-1 (AP-1) activity.
in vivo
I.c.v. injection of Senktide causes a dose-dependent increase in total distance traveled (F6,72=6.344, P<0.001). This increase reaches statistical significance compare to the vehicle-treated group at 0.06 nmol and higher. The Senktide-induced increase in locomotor activity brought about by 0.1 nmol of Senktide is significantly and dose-dependently decreased by the tachykinin NK3 receptor antagonists talnetant at 30 mg/kg and SB222200 at 30 mg/kg, but not by osanetant, when tested in parallel in a single experiment (F7,78=10.32, P<0.001), although a non-significant reduction is observed. However, when tested using another vehicle (Vitamin E and glycofurol), osanetant does decrease activity significantly compare to Senktide-treated gerbils (F2,30=10.10, P<0.001)[1].
