Corticotropin-releasing hormone (CRH) receptors in the mesenteric small arteries of rats resemble the (2)-subtype.
The potencies of the corticotropin-releasing hormone (CRH) agonistic peptides oCRH, h/rCRH, frog sauvagine, and carp urotensin I and of the antagonistic peptide alpha-helical CRH9-41 were compared in 3 different in vitro assays: (a) receptor binding to rat brain membranes; (b) release of ACTH/beta-endorphin from rat pituitary cells; and (c) relaxation of rat mesenteric small arteries. From their potency profiles, especially from the high potency of sauvagine relative to CRH in the relaxation assay, it is concluded that the receptors mediating the hypotensive action of systemic CRH in vascular smooth muscle are different from those in the pituitary and brain, and may be identical or very similar to the recently cloned new CRH receptor type 2.
Rohde
E
E
Research Institute of Molecular Pharmacology, Berlin, Germany.
Furkert
J
J
Fechner
K
K
Beyermann
M
M
Mulvany
M J
MJ
Richter
R M
RM
Denef
C
C
Bienert
M
M
Berger
H
H
D000324:Adrenocorticotropic Hormone / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive; D003346:Corticotropin-Releasing Hormone / Q000494:pharmacology*; D008297:Male; D008638:Mesenteric Arteries / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D018019:Receptors, Corticotropin-Releasing Hormone / Q000378:metabolism*
D018019:Receptors, Corticotropin-Releasing Hormone; D000324:Adrenocorticotropic Hormone; D003346:Corticotropin-Releasing Hormone