International Union of Pharmacology. XXXVI. Current Status of the Nomenclature for Receptors for Corticotropin-Releasing Factor and Their Ligands

High-Affinity CRF1 Receptor Antagonist NBI-34041: Preclinical and Clinical Data Suggest Safety and Efficacy in Attenuating Elevated Stress Response

“…These receptors have been termed the CRF 1 and the CRF 2 receptor with the CRF 2 receptor existing in three identified splice variant isoforms named CRF 2(a) , CRF 2(b), and CRF 2(c) (Hauger et al, 2003). Both receptor subtypes are found in human pituitary (Hiroi et al, 2001) and throughout the neocortex of primates (Sanchez et al, 1999), whereas in rodents only the CRF 1 receptor is expressed in pituitary and neocortex, and has a discrete localization with respect to the CRF 2 receptor (Chalmers et al, 1995).…”

CRF2 Receptor Deficiency Eliminates the Long-Lasting Vulnerability of Motivational States Induced by Opiate Withdrawal

“…For instance, CRF receptor antagonists reduce ethanol self-administration, the negative affective-like states of ethanol or cocaine withdrawal, and the stress-induced reinstatement of substance-seeking behavior in rats (Basso et al, 1999;Erb et al, 1998;Funk et al, 2006;Le et al, 2000;Shaham et al, 1997;Valdez et al, 2003). In mammals, CRF-like signaling is transmitted by two types of receptors, termed CRF 1 and CRF 2 (Hauger et al, 2003), that may differentially contribute to the multiple signs and symptoms of drug dependence and withdrawal. Indeed, CRF 1 or CRF 2 receptor deficiency completely eliminates the negative affective-like states of opiate withdrawal in mice (Contarino and Papaleo, 2005;Ingallinesi et al, 2012).…”

Urotensin I–CRF–Urocortins: A mermaid’s tail

“…The outcome of the work establishing a hormone family that, like the mermaid/merman, relates to the physiology of both humans and teleosts is far beyond what the original observations would have predicted. Thus, although we will present a succinct summary of the isolation, peptide chemistry, molecular pharmacology and physiology of the Urotensin I-CRF-Urocortin family and Urotensin II, we refer the reader to more comprehensive reviews of the subject for more detailed information (Davidson et al, 2009;Oki and Sasano, 2004;Hauger et al, 2003;Lu et al, 2008;Le Mével et al, 2008;Conlon, 2008 and see the May 2008 issue of Peptides, volume 29, devoted to Urotensin II topics). Further, although we will deal in brief with the co-discovery of Urotensin I and Urotensin II by the Bern and Lederis laboratories, in concert with the discovery of ovine CRF by the Vale laboratory, our focus will be primarily on Urotensin I.…”

“…Although the receptors responsible for the actions of UI and CRF were not known at the time the peptides were sequenced, it is now clear that the multiple activities of UI that had already been observed in a number of mammalian preparations (Lederis et al, 1985) are due to the activation of two homologous G-protein-coupled receptors, termed CRF 1 and CRF 2 (Hauger et al, 2003). There are three isoforms of CRF 2 (CRF 2a,2b,2c ) that differ in their Nterminal extracellular sequences, but not in their extracellular loops, transmembrane domains and intracellular sequences that are responsible for ligand binding and signal transduction, respectively.…”