Orexin receptor type 1

GWB-D39B30

Moderately selective excitatory receptor for orexin-A and with a lower affinity for orexin-B neuropeptide. Seems to be exclusively coupled to the G(q) subclass of heteromeric G proteins which activates the phospholipase C mediated signaling cascade (By similarity).

Belongs to the G-protein coupled receptor 1 family [view classification]. Summary: HCRTR1 or orexin 1 receptor (OX1R) is a G-protein coupled receptor expressed in the hypothalamus and involved in the regulation of feeding behaviour. HCRTR1 selectively binds the orexin A neuropeptide. It shares 64% identity with HCRTR2. [1] Ammoun S. Lindholm D. Wootz H. Akerman K. E. and Kukkonen J. P. et al. G-protein-coupled OX1 orexin/hcrtr-1 hypocretin receptors induce caspase-dependent and -independent cell death through p38 mitogen-/stress-activated protein kinase[2] Meerabux J. Iwayama Y. Sakurai T. Ohba H. Toyota T. Yamada K. Nagata R. Irukayama-Tomobe Y. Shimizu H. Yoshitsugu K. Ohta K. et al. Association of an orexin 1 receptor 408Val variant with polydipsia-hyponatremia in schizophrenic subjects[3] Spinazzi R. Rucinski M. Neri G. Malendowicz L. K. and Nussdorfer G. G. Preproorexin and orexin receptors are expressed in cortisol-secreting adrenocortical adenomas and orexins stimulate in vitro cortisol secretion and growth of tumor cells[4] Holmqvist T. Johansson L. Ostman M. Ammoun S. Akerman K. E. and Kukkonen J. P. OX1 orexin receptors couple to adenylyl cyclase regulation via multiple mechanisms[5] Karteris E. Chen J. and Randeva H. S. et al. Expression of human prepro-orexin and signaling characteristics of orexin receptors in the male reproductive system[6] Sakurai T. Amemiya A. Ishii M. Matsuzaki I. Chemelli R. M. Tanaka H. Williams S. C. Richardson J. A. Kozlowski G. P. Wilson S. et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. [7] Hungs M. Mignot E. Hypocretin/orexin sleep and narcolepsy. [8] Willie J. T. Chemelli R. M. Sinton C. M. Yanagisawa M. To eat or to sleep? Orexin in the regulation of feeding and wakefulness.