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In this study we demonstrate a new role of MRAP2 in the regulation of the orexin receptor 1 (OX1R) and identify the specific regions of MRAP2 required for the regulation of OX1R and PKR1 (show PROKR1 Proteins). Importantly, like MC4R (show MC4R Proteins) and PKRs, OX1R is predominately expressed in the brain where it regulates food intake
After sequencing all orexin receptor exons, one variation (rs2271933) in the OX1R gene and one variation (rs2653349) in the OX2R (show HCRTR2 Proteins) gene were found. However, no significant differences were found in either genotypic or allelic frequency distributions between the two study groups
G-protein-dependency of OX1 (show NQO1 Proteins) receptor signalling
Several single nucleotide polymorphisms (SNPs) in HCRTR2 (show HCRTR2 Proteins) were nominally associated with Antipsychotic-induced weight gain (AIWG) in patients of European ancestry treated with either clozapine or olanzapine. None of the SNPs in HCRTR1 were associated with AIWG.
Rapid-onset obesity with hypothalamic dysfunction, hypoventilation, and autonomic dysregulation is highly unlikely to be caused by mutations in the exons of the HCRTR1 gene.
This study determined structures of OX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-A and 2.75-A resolution.
the orexinA/OX1 (show NQO1 Proteins) receptor axis has a significant pro-survival function in adrenal cells.
OX1R signaling can attenuate KOR (show OPRK1 Proteins)-mediated reduction of cellular cAMP levels while enhancing KOR (show OPRK1 Proteins)-mediated beta-arrestin recruitment and p38 (show CRK Proteins) activation.
OX1R and KOR (show OPRK1 Proteins) heterodimerize, and this heterodimer associates with Galphas (show GNAS Proteins), leading to increased protein kinase A (PKA) signaling pathway activity, including upregulation of intracellular cAMP levels.
Results from homology and docking modeling show two alternative binding modes for orexin-A into orexin 1 receptor in concordance with what is known of G protein coupled receptors activation in general and the mutational data.
Investigated the role of orexin receptors in compulsive-like alcohol drinking, found that systemic administration of the selective OX1R blocker SB-334867 reduced compulsive-like consumption. Results suggest that OX1R signaling is particularly important for promoting compulsive-like alcohol drinking, and that OX1Rs might represent a novel therapy to counteract compulsive aspects of human alcohol use disorders.
OXA and OX1R are expressed in the testis and that they may help in proliferation and development of germ cells, Leydig cells and Sertoli cells, and in the spermatogenic process and steroidogenesis.
Results thus suggest that type 1 diabetes mellitus impairs testicular steroidogenesis and glucose homeostasis through inhibition of orexin A/OX1R signaling cascade due to decreased OX1R expression in adult mice, thereby affecting germ cell survival and their proliferation in the testis.
Binding of OXA to OX1R is important for the development of the testis.
Study demonstrated that activation of the OX1 (show NQO1 Proteins) receptor in the ventrolateral periaqueductal gray of mice can initiate an endocannabinoid-CB1 (show CNR1 Proteins) receptor-mediated analgesia. Activation of the OX2 receptor (show CD200R1 Proteins) in the ventrolateral periaqueductal gray was also antinociceptive but this antinociceptive effect is CB1 (show CNR1 Proteins) receptor-independent.
Elevation levels of OX1R and OX2R (show CD200R1 Proteins) following experimental autoimmune encephalomyelitis induction suggest that alteration in orexinergic system may involve in pathogenesis of multiple sclerosis.
Study provides pharmacological and molecular evidence indicating, respectively, a role for OXR1 (show OXR1 Proteins) signaling in ethanol and saccharin binge-like drinking
orexin activation of OX1R in the bone locally suppresses bone formation and enhances bone resorption by lowering osseous ghrelin (show GHRL Proteins) expression.
findings demonstrate that Hcrtr-1 modulates the reinforcing properties of cannabinoids.
The transcripts for the Orx1 and Orx2 receptors diverged in the basolateral amygdala with Orx1 increasing and Orx2 decreasing in animals that were susceptible to the chronic defeat.
39 of 41 in: Acta Histochem. 2014 Jan;116(1) Orexin 1 receptor is expressed in the seminiferous tubules of boar testis.
Immunoreactivity (IR) for both orexins A and B (OXA and OXB), and cognate receptors (OX1R and OX2R (show HCRTR2 Proteins)) were identified only in the excretory striated (show NSDHL Proteins) ducts of the MSG while acinar cells were not immunoreactive.
Data demonstrated the presence of OX1R and OX2R (show HCRTR2 Proteins) genes and proteins in the ovary of the pig and the impact of the hormonal milieu on the expression of both receptors.
expression of OX1R and Ox2R (show HCRTR2 Proteins) in hypothalamus during oestrous cycle; evidence OX1R and OX2R (show HCRTR2 Proteins) mRNAs and proteins occur in hypothalamic structures engaged in control of reproduction; indicate dependence of OXR expression on endocrine reproductive state
findings provide the first evidence that orexin receptors 1 and 2 messenger RNAs and proteins occur in the pituitary of the pig and indicate the dependence of orexin receptor expression on the endocrine reproductive state
These data confirmed expression of orexin and its two receptors in the bovine adrenal gland.
first evidence for the expression of oxA and ox1R in the vestibular glands of mammalian genital tract
The protein encoded by this gene is a G-protein coupled receptor involved in the regulation of feeding behavior. The encoded protein selectively binds the hypothalamic neuropeptide orexin A. A related gene (HCRTR2) encodes a G-protein coupled receptor that binds orexin A and orexin B.
hypocretin receptor 1
, hypocretin receptor type 1
, hypocretin receptor-1
, orexin receptor 1
, orexin receptor type 1
, orexin receptor-1
, hypocretin (orexin) receptor 1
, orexin receptor type 1-like