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RP 67580

Names

[ CAS No. ]:
135911-02-3

[ Name ]:
RP 67580

[Synonym ]:
Tocris-1635
RP-67580

Biological Activity

[Description]:

RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[In Vivo]

RP 67580（0.03-1 mg/kg；静脉注射；单剂量）显著抑制神经源性炎症。 Animal Model: Male albino Sprague-Dawley rats Dosage: 0.03, 0.1, 0.3, 1 mg/kg Administration: i.v.; single dose Result: Potently and dose-dependently inhibited the strong plasma extravasation caused by electrical stimulation of the saphenous nerve for 15 minutes with an ED50 value of 0.15 mg/kg.

[References]

[1]. Garret C, et al. Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc Natl Acad Sci U S A. 1991 Nov 15;88(22):10208-12.  

Chemical & Physical Properties

[ Density]:
1.17 g/cm3

[ Boiling Point ]:
588.5ºC at 760 mmHg

[ Melting Point ]:
195-188ºC

[ Molecular Formula ]:
C29H30N2O2

[ Molecular Weight ]:
438.56

[ Flash Point ]:
309.7ºC

[ Exact Mass ]:
438.23100

[ PSA ]:
53.39000

[ LogP ]:
5.14980

[ Vapour Pressure ]:
7.89E-14mmHg at 25°C

[ Index of Refraction ]:
1.626

Related Compounds