GR 64349

Names

[ Name ]:
GR 64349

[Synonym ]:
1-Lithio-2-methylnaphthalin, lithium
1-lithio-2-methylnaphthalene

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]:

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.

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

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.