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G114

Sigma-Aldrich

GR 73632

>97%

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About This Item

Fórmula empírica (notación de Hill):
C40H59N7O6S
Número de CAS:
133156-06-6
Peso molecular:
766.00
MDL number:
MFCD00144411
UNSPSC Code:
12352202
PubChem Substance ID:
329799741
NACRES:
NA.32

assay

>97%

storage temp.

−20°C

SMILES string

CSCC[C@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H]1CCCN1C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCCCN)C(N)=O

InChI

1S/C40H59N7O6S/c1-27(2)24-34(38(51)44-30(36(42)49)20-23-54-4)46(3)40(53)33-18-13-22-47(33)39(52)32(26-29-16-9-6-10-17-29)45-37(50)31(25-28-14-7-5-8-15-28)43-35(48)19-11-12-21-41/h5-10,14-17,27,30-34H,11-13,18-26,41H2,1-4H3,(H2,42,49)(H,43,48)(H,44,51)(H,45,50)/t30-,31-,32-,33-,34-/m0/s1

InChI key

HQKPTSSZOJLFBZ-LJADHVKFSA-N

Gene Information

human ... TAC1(6863) , TACR1(6869)
mouse ... TAC1(21333) , TACR1(21336)
rat ... TAC1(24806) , TACR1(24807)

Amino Acid Sequence

H2N-(CH2)4-CO-Phe-Pro-NMe-Leu-Met-NH2

General description

Neurokinin (NK) receptors are acted upon by tachykinins or neurokinins namely, NKA and NKB. These are endogenous ligands. An exogenous agonist/ligand for NK1 is GR 64349 petpide.

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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M L Woolley et al.
Brain research, 1078(1), 151-158 (2006-02-24)
Identification of the selective neurokinin NK(1) receptor antagonist, 2-(R)-(1-(R)-3,5-Bis(trifluromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5yl)methylmor-phine (MK-869), as a novel therapeutic approach for anxiety/depression has led to increased use of the Mongolian gerbil in behavioural studies since the gerbil NK(1) receptor pharmacology is similar to human, but
J M Hall et al.
British journal of pharmacology, 102(2), 511-517 (1991-02-01)
1. This study investigated the recognition characteristics of neurokinin receptors mediating potentiation of the contractile response to field stimulation in the guinea-pig vas deferens. 2. A predominant NK1 receptor population is strongly suggested by the relative activities of the common
Andrew P Ray et al.
Behavioral neuroscience, 123(3), 701-706 (2009-06-03)
The neurocircuitry mediating the emetic reflex is still incompletely understood, and a key question is the degree to which central and/or peripheral components contribute to the overall vomiting mechanism. Having previously found a significant peripheral component in neurokinin NK-receptor mediated
Nissar A Darmani et al.
Pharmacology, biochemistry, and behavior, 99(4), 573-579 (2011-06-21)
Significant electrophysiological and biochemical findings suggest that receptor cross-talk occurs between serotonergic 5-HT(3)- and tachykininergic NK(1)-receptors in which co-activation of either receptor by ineffective doses of their corresponding agonists (serotonin (5-HT) or substance P (SP), respectively) potentiates the activity of
Takako Yoshino-Furukawa et al.
Biological & pharmaceutical bulletin, 36(1), 76-81 (2013-01-11)
The pharmacological properties of the novel neurokinin-1 (NK(1)) receptor antagonist FK886, ([3,5-bis(trifluoromethyl)phenyl][(2R)-2-(3-hydroxy-4-methylbenzyl)-4-{2-[(2S)-2-(methoxymethyl)morpholin-4-yl]ethyl}piperazin-1-yl]methanone dihydrochloride), were studied. FK886 potently inhibited the binding of [(125)I]Bolton-Hunter-labeled substance P ([(125)I]BH-SP; 100 pM) to human NK(1) receptors expressed in Chinese hamster ovary (CHO) cells (IC(50)=0.70 nM). It also
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