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...