GR 64349

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

GR 64349 Structure
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].

 Names

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

 GR 64349 Biological Activity

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
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.

 Chemical & Physical Properties

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

 Safety Information

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

 Articles3

More Articles
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...

 Synonyms

1-Lithio-2-methylnaphthalin, lithium
1-lithio-2-methylnaphthalene
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