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CRF Receptors
Corticotropin-releasing factor (CRF), also known as corticotropin-releasing hormone, is a major regulator of homeostasis, mediating the autonomic, behavioral and neuroendocrine responses to stress. CRF has also been suggested to play a role in cell growth and survival. To date, two types of CRF receptors have been cloned from several mammals: CRF1 and CRF2 receptors. Two splice variants of the CRF2 receptor have been identified in rodents; CRF2a and CRF2b.
CRF Receptor Target Files
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The tables below summarizes the properties of these receptors and include examples of selective ligands available from Tocris.
| Receptor Subtype | CRF1 | CRF2a | CRF2b |
|---|
| Transduction Mechanism | Activates Gs | Activates Gs | Activates Gs |
| Key Compounds | Ki (nM) |
|---|
| Agonists |
CRF (human, rat) (1151) Urocortin (rat) (1605) Sauvagine (1609) Stressin I (1608) |
11 13 9.4 1.5 |
44 1.5 9.9 224 |
38 0.97 3.8 224 |
| Antagonists |
Astressin (1606) α-helical CRF 9-41 (1184) NBI 27914 (1591) CP 154526 (2779) CP 376395 (3212) K 41498 (2070) |
2 17 2 2.7 12 425 |
1.5 5 > 10000 > 10000 > 10000 0.66 |
1 0.97 - > 10000 > 10000 0.62 |
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7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
Antidepressants - Current and Future Targets
Written by P. Skolnich et al
'Antidepressants - Current and Future Targets' provides an overview of the current and future targets for the treatment of major depressive disorder.
Gut Hormones and the Regulation of Appetite
Written by V.J. Taylor et al
'Gut Hormones and the Regulation of Appetite' summarizes the neuropeptide modulators and gut hormones that influence appetite
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