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G114

Sigma-Aldrich

GR 73632

>97%

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About This Item

Empirische Formel (Hill-System):
C40H59N7O6S
CAS-Nummer:
133156-06-6
Molekulargewicht:
766.00
MDL-Nummer:
MFCD00144411
UNSPSC-Code:
12352202
PubChem Substanz-ID:
329799741
NACRES:
NA.32

Assay

>97%

Lagertemp.

−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

InChIKey

HQKPTSSZOJLFBZ-LJADHVKFSA-N

Angaben zum Gen

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

Allgemeine Beschreibung

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. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)

Analysenzertifikate (COA)

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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
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
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
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
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
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