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PubMed: 8940412

Title
In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation.
Journal
Endocrinology
Volume
137
Issue
None
Pages
5747-50
Date
1996-12-01
Authors
Chrousos GP | Lewis DB | Rice KC | Torpy DJ | Webster EL | Zachman EK

Evidence 0c59fd5b3a
JSON

Antalarmin potently displaced 1251-oCRH binding, exhibiting respectively Ki values of 1. 9 f 0.9,. 1.3 f .4, and 1.4 f .6 nM (mean f SEM) in pituitary, cerebellum, and frontal cortex homogenates.Antalarmin, by effectively displacing IoCRH binding in tissues predominately expressing CRHRl but not in tissues expressing CRHR2, appears to be a specific CRHRl receptor antagonist.

a(CHEBI:antalarmin) directlyDecreases act(p(RGD:Crh)) View Subject | View Object

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Annotations
Uberon
pituitary gland

a(CHEBI:antalarmin) directlyDecreases act(p(RGD:Crhr1)) View Subject | View Object

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Annotations
Uberon
pituitary gland

act(p(RGD:Crh)) directlyIncreases act(p(RGD:Crhr1)) View Subject | View Object

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Annotations
Uberon
pituitary gland

Evidence 5a4bec57c8
JSON

These results raise the possibility that pyrrolopyrimidine compounds, such as antalarmin, which antagonize CRH at the level of its own receptor, have therapeutic potential in some forms of inflammation.

a(CHEBI:antalarmin) negativeCorrelation bp(GO:"inflammatory response") View Subject | View Object

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bp(GO:"inflammatory response") negativeCorrelation a(CHEBI:antalarmin) View Subject | View Object

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Evidence b2909476c3
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Indeed, the compound significantly suppressed (XI-l-induced ACTH secretion to approximately the same extent as neutralizing polyclonal anti-CRH.

a(CHEBI:antalarmin) decreases sec(p(RGD:Pomc)) View Subject | View Object

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Evidence a1549da5a6
JSON

Corticotropin-releasing hormone (CRH) secreted from the hypothalamus is the major regulator of pituitary ACTH release and consequent glucocorticoid secretion. CRH secreted in the periphery also acts as a proinflammatory modulator.

bp(GO:"inflammatory response") positiveCorrelation act(p(RGD:Crh)) View Subject | View Object

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act(p(RGD:Crh)) positiveCorrelation bp(GO:"inflammatory response") View Subject | View Object

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act(p(RGD:Crh)) regulates sec(p(RGD:Pomc)) View Subject | View Object

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