G114
GR 73632
>97%
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关于此项目
经验公式（希尔记法）:
C40H59N7O6S
化学文摘社编号:
分子量:
766.00
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352202
MDL number:
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
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 key
HQKPTSSZOJLFBZ-LJADHVKFSA-N
assay
>97%
storage temp.
−20°C
Gene Information
human ... TAC1(6863), TACR1(6869)
mouse ... TAC1(21333), TACR1(21336)
rat ... TAC1(24806), TACR1(24807)
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
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
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
Monika Sundqvist et al.
European journal of pharmacology, 577(1-3), 78-86 (2007-10-09)
Intracerebroventricular (i.c.v.) administration of tachykinin NK(1) receptor agonists induces tapping of the hind legs in gerbils, so-called gerbil foot tapping, which is thought to reflect a fear-related response. The aim of the present study was to examine how ligands selective
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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