GR 64349

Modify Date: 2024-01-02 12:37:19

GR 64349 structure	Common Name	GR 64349
	CAS Number	137593-52-3	Molecular Weight	921.11500
	Density	1.31g/cm3	Boiling Point	1342.8ºC at 760mmHg
	Molecular Formula	C₄₂H₆₈N₁₀O₁₁S	Melting Point	N/A
	MSDS	USA	Flash Point	765.9ºC

Use of GR 64349

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively[1][2].

Name	L-lysyl-L-α-aspartyl-L-seryl-L-phenylalanyl-L-valyl-(αS,3R)-3-amino-α-(2-methylpropyl)-2-oxo-1-pyrrolidineacetyl-L-methioninamide
Synonym	More Synonyms

Description	GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively[1][2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor
References	[1]. Y Chang, et al. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J Pharmacol Exp Ther. 2000 Jul;294(1):147-54. [2]. M J Deal, et al. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J Med Chem. 1992 Oct 30;35(22):4195-204.

Description

Related Catalog

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

References

[1]. Y Chang, et al. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J Pharmacol Exp Ther. 2000 Jul;294(1):147-54.

[2]. M J Deal, et al. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J Med Chem. 1992 Oct 30;35(22):4195-204.

Density	1.31g/cm3
Boiling Point	1342.8ºC at 760mmHg
Molecular Formula	C₄₂H₆₈N₁₀O₁₁S
Molecular Weight	921.11500
Flash Point	765.9ºC
Exact Mass	920.47900
PSA	372.87000
LogP	1.98680

GR 64349 MSDS(Chinese)

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR	NONH for all modes of transport

(R)-2-(3-((tert...

CAS#:124202-00-2

GR 64349

CAS#:137593-52-3

Literature: Deal, Martyn J.; Hagan, Russell M.; Ireland, Simon J.; Jordan, Christopher C.; McElroy, Andrew B.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4195 - 4204

boc-freidinger'...

CAS#:82611-48-1

GR 64349

CAS#:137593-52-3

Literature: Deal, Martyn J.; Hagan, Russell M.; Ireland, Simon J.; Jordan, Christopher C.; McElroy, Andrew B.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4195 - 4204

N-(tert-butoxyc...

CAS#:82611-46-9

GR 64349

CAS#:137593-52-3

Literature: Deal, Martyn J.; Hagan, Russell M.; Ireland, Simon J.; Jordan, Christopher C.; McElroy, Andrew B.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4195 - 4204

Fmoc-Val-OPfp

CAS#:86060-87-9

Fmoc-Phe-OPfp

CAS#:86060-92-6

Fmoc-Met-OH

CAS#:71989-28-1

N/A

CAS#:143267-21-4

Detail

Literature: Deal, Martyn J.; Hagan, Russell M.; Ireland, Simon J.; Jordan, Christopher C.; McElroy, Andrew B.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4195 - 4204

Precursor 5
CAS#:82611-48-1 boc-freidinger'... CAS#:82611-46-9 N-(tert-butoxyc... CAS#:86060-87-9 Fmoc-Val-OPfp CAS#:86060-92-6 Fmoc-Phe-OPfp
CAS#:71989-28-1 Fmoc-Met-OH
DownStream 0

Endogenous modulation of excitatory amino acid responsiveness by tachykinin NK1 and NK2 receptors in the rat spinal cord.

Br. J. Pharmacol. 115(6) , 1013-9, (1995)

1. The effects of selective tachykinin (neurokinin, NK) NK1 and NK2 receptor antagonists have been examined on spinal neurones in alpha-chloralose anaesthetized, spinalized rats. They were tested for ...

Tachykinin receptor types: Classification and membrane signalling mechanisms.

Neurochem. Int. 18 , 149-165, (1991)

The use of selective agonists in both functional and binding studies has provided unequivocal evidence for the existence of three types of tachykinin receptor (NK(1), NK(2) and NK(3)); there is also p...

Receptor-selective, peptidase-resistant agonists at neurokinin NK-1 and NK-2 receptors: new tools for investigating neurokinin function.

Neuropeptides 19 , 127-135, (1991)

The pharmacological profiles of two novel neurokinin agonists have been investigated. delta Ava[L-Pro9,N-MeLeu10]SP(7-11) (GR73632) and [Lys3,Gly8-R-gamma-lactam-Leu9] NKA(3-10) (GR64349) are potent a...

1-Lithio-2-methylnaphthalin, lithium

1-lithio-2-methylnaphthalene

GR 64349

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