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G114

Sigma-Aldrich

GR 73632

>97%

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About This Item

Empirical Formula (Hill Notation):
C40H59N7O6S
CAS Number:
133156-06-6
Molecular Weight:
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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Adri van den Hoogenband et al.
Bioorganic & medicinal chemistry letters, 16(4), 1045-1048 (2005-11-18)
The synthesis and structure-activity relations for a new class of centrally active NK-1 receptor antagonists are described. The new compounds are based on piperazine 2 and contain an oxime ether functionality. Several new compounds have high affinity for the NK-1
He-Bin Tang et al.
Molecular pain, 3, 42-42 (2007-12-26)
Although substance P (SP) is an important primary afferent modulator in nociceptive processes, it is unclear whether SP regulates its own release from primary sensory neurons. Using a highly sensitive radioimmunoassay for SP, we have demonstrated that the activation of
J M Hall et al.
European journal of pharmacology, 199(1), 9-14 (1991-06-18)
We have used novel selective agonist ligands to examine neurokinin receptors mediating the contractile response to tachykinins in the rabbit iris sphincter preparation in vitro. The selective NK-1 receptor agonist delta-amino valeryl-[L-Pro9,N-Me Leu10]SP-(7-11) (GR73632) and the NK-3 receptor-selective agonist succ-[Asp6,N-Me-Phe8]
Nissar A Darmani et al.
Brain research, 1214, 58-72 (2008-05-13)
Substance P (SP) is thought to play a cardinal role in emesis via the activation of central tachykinin NK1 receptors during the delayed phase of vomiting produced by chemotherapeutics. Although the existing supportive evidence is significant, due to lack of
Johannes Tauscher et al.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, 20(2), 80-87 (2009-12-19)
The neurokinin-1 (NK-1) antagonist LY686017 showed activity in preclinical anxiety models. The clinical development of LY686017 included a PET study and a proof-of-concept in social anxiety disorder (SAD). [(11)C]GR205171 was used healthy volunteers receiving 1-100mg/d LY686017 for 28 days to
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