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CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. 1996

D W Schulz, and R S Mansbach, and J Sprouse, and J P Braselton, and J Collins, and M Corman, and A Dunaiskis, and S Faraci, and A W Schmidt, and T Seeger, and P Seymour, and F D Tingley, and E N Winston, and Y L Chen, and J Heym
Department of Neuroscience, Pfizer Central Research, Groton, CT 06340, USA.

Here we describe the properties of CP-154,526, a potent and selective nonpeptide antagonist of corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (Ki < 10 nM) and blocks CRF-stimulated adenylate cyclase activity in membranes prepared from rat cortex and pituitary. Systemically administered CP-154,526 antagonizes the stimulatory effects of exogenous CRF on plasma ACTH, locus coeruleus neuronal firing and startle response amplitude. Potential anxiolytic activity of CP-154,526 was revealed in a fearpotentiated startle paradigm. These data are presented in the context of clinical findings, which suggest that CRF is hypersecreted in certain pathological states. We propose that a CRF antagonist such as CP-154,526 could affirm the role of CRF in certain psychiatric diseases and may be of significant value in the treatment of these disorders.

UI MeSH Term Description Entries
D007276 Injections, Intraventricular Injections into the cerebral ventricles. Intraventricular Injections,Injection, Intraventricular,Intraventricular Injection
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008125 Locus Coeruleus Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY. Locus Caeruleus Complex,Locus Caeruleus,Locus Ceruleus,Locus Ceruleus Complex,Locus Coeruleus Complex,Nucleus Pigmentosus Pontis,Caeruleus Complex, Locus,Complex, Locus Caeruleus,Complex, Locus Ceruleus,Complex, Locus Coeruleus,Pontis, Nucleus Pigmentosus
D008297 Male Males
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D010902 Pituitary Gland A small, unpaired gland situated in the SELLA TURCICA. It is connected to the HYPOTHALAMUS by a short stalk which is called the INFUNDIBULUM. Hypophysis,Hypothalamus, Infundibular,Infundibular Stalk,Infundibular Stem,Infundibulum (Hypophysis),Infundibulum, Hypophyseal,Pituitary Stalk,Hypophyseal Infundibulum,Hypophyseal Stalk,Hypophysis Cerebri,Infundibulum,Cerebri, Hypophysis,Cerebrus, Hypophysis,Gland, Pituitary,Glands, Pituitary,Hypophyseal Stalks,Hypophyses,Hypophysis Cerebrus,Infundibular Hypothalamus,Infundibular Stalks,Infundibulums,Pituitary Glands,Pituitary Stalks,Stalk, Hypophyseal,Stalk, Infundibular,Stalks, Hypophyseal,Stalks, Infundibular
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D011758 Pyrroles Azoles of one NITROGEN and two double bonds that have aromatic chemical properties. Pyrrole
D002144 Callithrix A genus of the subfamily CALLITRICHINAE occurring in forests of Brazil and Bolivia and containing seventeen species. Callithrix jacchus,Hapale,Marmoset, Common,Marmoset, Short-Tusked,Marmosets,Common Marmoset,Common Marmosets,Marmoset,Marmoset, Short Tusked,Short-Tusked Marmoset,Short-Tusked Marmosets
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell

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