Tachykinins

Ascending pain pathways. IL: intralaminar nucleus of the thalamus, VP: ventroposterior nucleus of the thalamus.

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A5330 N-Acetyl-L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester ≥99% (TLC), powder Competitive substance P receptor antagonist. It is approximately 1000-fold more potent at cloned human NK-1 receptors than at cloned human NK-2 and NK-3 receptors; and approximately 200-fold more potent at human NK-1 receptors than at rat NK-1 receptors. The IC50 for the human NK-1 receptor expressed in CHO cells is approximately 2 nM.
PZ0136 CP-100263 dihydrochloride hydrate ≥97% (HPLC) CP-100263 is an NK-1 neurokinin receptor antagonist.
C9373 CP-96345 ≥98% (HPLC) CP-96345 is a selective NK1 antagonist. CP96345 inhibits substance P-induced salivation in the rat by classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors.
SML0752 (+)-CP-99994 dihydrochloride ≥98% (HPLC) (+)-CP-99994 is a selective neurokinin (NK)-1 tachykinin antagonist. (+)-CP-99994 binds selectively and with high affinity with a Ki of 0.25 nM in a human cell line.
SML0780 GR203040 ≥98% (HPLC) GR203040 is a high affinity, non-peptide tachykinin NK1 receptor antagonist. GR203040 inhibits substance P binding to human NK1 receptors in CHO cells with a pKi or 10.3. The compound prevents emisis, and reduces bladder damage induced by radiation, cisplatin and cyclophosphamide. 11C-labeled GR203040 is used as a radioligand to image NK1 receptors in the CNS by PET scanning.
G113 GR 64349 >96% GR 64349 peptide acts as an agonist of neurokinin (NK2) receptor, which leads to reduced NK2 response to kainate and AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid), but not to NMDA (N-methyl-D-aspartate).
G114 GR 73632 >97% GR 73632 interacts with neurokinin (NK1) receptor, which results in rhythmic tapping of hind-foot in gerbils. Administration of this peptide in the intra-ventral tegmental area (VTA) results in locomotor activity. It interacts with and activates NK1 receptors present on smooth muscle and interstitial cells of Cajal, resulting in elevated distention-induced peristalsis.
H1664 Hemokinin 1 human ≥98% (HPLC), solid Hemokinin 1 (HK1) is an endogenous agonist for all tachykinin receptors. However, it is highly selective for the NK1 (neurokinin 1) receptor. HK1 and substance-P compete with each other for binding to NK1. HK1 is involved in the B-cell as well as T-cell development.
NK1 tachykinin receptor agonist.
H0409 Hylambatin >96% (HPLC) Tachykinin that increases plasma glucose and plasma insulin.
L119 L-703,606 oxalate salt hydrate solid Potent and selective non-peptide NK-1 tachykinin receptor antagonist.
L138 L-733,061 hydrochloride solid Weak NK-1 tachykinin receptor antagonist; less active enantiomer of L-733,060 hydrochloride.
M157 MEN-10,376 ≥95% (HPLC), solid Potent and selective NK-2 tachykinin receptor antagonist.
N4267 Neurokinin A ≥97% (HPLC) Endogenous tachykinin agonist with preference for the NK-2 receptor, more potent bronchoconstrictor than Substance P.
N4143 Neurokinin B ≥95% (HPLC) Endogenous tachykinin agonist with preference for the NK-3 receptor. Potent bronchoconstrictor; may have neuromodulatory role in brain.
SML0798 Osanetant ≥98% (HPLC) Osanetant is a selective antagonist of neurokinin 3 receptor NK3. 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 that 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. Osanetant was in clinical trials for both irritable bowel syndrome and schizophrenia.
S5192 SB 222200 ≥98% (HPLC), solid Non-peptide NK3 tachykinin receptor antagonist.
SB 222200 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
SML0764 Senktide trifluoroacetate salt ≥95% (HPLC) 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 that 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.
S6883 Substance P acetate salt hydrate ≥95% (HPLC), powder NK-1 agonist; potent vasodilator and hypotensive agent; induces salivation; increases capillary permeability; induces mast cell degranulation; putative neurotransmitter in sensory (pain) afferents.
S3144 [D-Arg1, D-Phe5, D-Trp7,9, Leu11]-Substance P ≥95% (HPLC) NK-1 tachykinin receptor antagonist
S3672 [Sar9, Met(O2)11]-Substance P ≥95% (HPLC) Highly selective NK-1 receptor agonist.
S2275 Acetyl-[Arg6, Sar9, Met(O2)11]-Substance P Fragment 6-11 ≥95% Selective NK-1 receptor agonist.
SML1165 Talnetant ≥98% (HPLC) Talnetant (SB-223,412) is a highly selective antagonist of neurokinin 3 receptor with a Ki (NK3) = 1 nM >10000 (NK1) >140 (NK2). 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 that 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. Talnetant was in clinical trials for both irritable bowel syndrome and schizophrenia.
W103 WIN 51708 hydrate solid WIN 51708 hydrate is a non-peptide NK1 tachykinin receptor antagonist.
W104 WIN 62,577 solid Non-peptide NK1 tachykinin receptor antagonist.