Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist

S McLean; A H Ganong; T F Seeger; D K Bryce; K G Pratt; L S Reynolds; C J Siok; J A Lowe 3rd; J Heym

doi:10.1126/science.1703324

Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist

Science. 1991 Jan 25;251(4992):437-9. doi: 10.1126/science.1703324.

Authors

S McLean¹, A H Ganong, T F Seeger, D K Bryce, K G Pratt, L S Reynolds, C J Siok, J A Lowe 3rd, J Heym

Affiliation

¹ Department of Neuroscience, Central Research Division, Pfizer Inc., Groton, CT 06340.

PMID: 1703324
DOI: 10.1126/science.1703324

Abstract

CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK1 receptor. The compound binds to a single population of sites in guinea pig brain and potently inhibits substance P-induced excitation of locus ceruleus neurons. CP-96,345 should be a useful tool for studying the action of substance P in the central nervous system.

MeSH terms

Action Potentials
Animals
Autoradiography
Binding Sites
Binding, Competitive
Biphenyl Compounds / metabolism*
Biphenyl Compounds / pharmacology
Brain / diagnostic imaging
Brain / metabolism*
Corpus Striatum / diagnostic imaging
Corpus Striatum / metabolism*
Guinea Pigs
Hydrogen-Ion Concentration
Male
Radionuclide Imaging
Receptors, Neurokinin-1
Receptors, Neurotransmitter / antagonists & inhibitors*
Receptors, Neurotransmitter / metabolism*
Receptors, Tachykinin
Spectrophotometry
Substance P / metabolism
Tachykinins / metabolism

Substances

Biphenyl Compounds
Receptors, Neurokinin-1
Receptors, Neurotransmitter
Receptors, Tachykinin
Tachykinins
Substance P
CP 96345