A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity

A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits... The multiple actions of corticotropin-releasing factor (CRF) on neuroendocrine and behavioural functions can now be examined using new, high affinity, non peptidic antagonists which exhibit central activity upon systemic application. We have shown that compound CP 154,526 (butyl-ethyl-(2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7 H -pyrrolo(2,3- d )pyrimidin-4-yl)amine) displaces ( 125 I)(Tyr 0 )CRF from rat hippocampal CRF receptors (IC 50 = 0.5 nM) and from pituitary CRF receptors (IC 50 = 0.04 nM). The same compound inhibits in a concentration-dependent manner the ovine CRF (0.1 μM)-stimulated adenylate cyclase activity in membranes of a mouse pituitary adenoma cell line, AtT20, with an IC 50 value of 50 nM. Systemic application of the CRF receptor antagonist (0.16 mg/kg i.p.) blocked recombinant human interleukin-1β (5 μg/kg i.p.) induced fever in rats. The CRF receptor antagonist CP 154,526 (1 mg/kg i.p.) also exhibited signs of anxiolytic-like activity in the elevated plus-maze test in rats. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png European Journal of Pharmacology Elsevier

A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity

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Publisher
Elsevier
Copyright
Copyright © 1996 Elsevier Ltd
ISSN
0014-2999
DOI
10.1016/0014-2999(96)00337-8
Publisher site
See Article on Publisher Site

Abstract

The multiple actions of corticotropin-releasing factor (CRF) on neuroendocrine and behavioural functions can now be examined using new, high affinity, non peptidic antagonists which exhibit central activity upon systemic application. We have shown that compound CP 154,526 (butyl-ethyl-(2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7 H -pyrrolo(2,3- d )pyrimidin-4-yl)amine) displaces ( 125 I)(Tyr 0 )CRF from rat hippocampal CRF receptors (IC 50 = 0.5 nM) and from pituitary CRF receptors (IC 50 = 0.04 nM). The same compound inhibits in a concentration-dependent manner the ovine CRF (0.1 μM)-stimulated adenylate cyclase activity in membranes of a mouse pituitary adenoma cell line, AtT20, with an IC 50 value of 50 nM. Systemic application of the CRF receptor antagonist (0.16 mg/kg i.p.) blocked recombinant human interleukin-1β (5 μg/kg i.p.) induced fever in rats. The CRF receptor antagonist CP 154,526 (1 mg/kg i.p.) also exhibited signs of anxiolytic-like activity in the elevated plus-maze test in rats.

Journal

European Journal of PharmacologyElsevier

Published: Aug 8, 1996

References

  • Mediation by corticotropin releasing factor (CRF) of adenohypophysial hormone secretion
    Rivier, C.L.; Plotsky, P.M.

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