Orexin receptors in GtoPdb v.2023.1

نویسندگان

چکیده

Orexin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on [43]) are activated endogenous polypeptides orexin-A and orexin-B (also known hypocretin-1 -2; 33 28 aa) derived from a common precursor, preproorexin or orexin proteolytic cleavage some typical peptide modifications [117]. signaling has been associated with regulation of sleep wakefulness, reward addiction, appetite feeding, pain gating, stress response, anxiety depression. Currently receptor ligands in clinical use dual antagonists suvorexant lemborexant daridorexant, which used hypnotics, several OX2-selective under development. Multiple agonists development for treatment narcolepsy other disorders. 3D structures have solved [146, 144, 55, 126, 47, 109, 7, 145].

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Orexin and Orexin Receptors

“Reverse pharmacology”, i.e., ligand identification using cell lines expressing orphan receptors, combined with genetic engineering techniques, has increased our understanding of novel signaling systems in the body. Orexin is the first and most successful example of the factors to which such an approach was applied. Our group initially identified orexin A and orexin B as endogenous peptide liga...

متن کامل

Multiple signaling pathways of orexin receptors

MicroRNAs (miRNAs) are short, 22–25 nucleotide long transcripts that may suppress entire signaling pathways by interacting with the 3’-untranslated region (3’-UTR) of coding mRNA targets, interrupting translation and inducing degradation of these targets. The long 3’-UTRs of brain transcripts compared to other tissues predict important roles for brain miRNAs. Supporting this notion, we found th...

متن کامل

Integrative physiology of orexins and orexin receptors.

Recent studies have established that the orexin system is a critical regulator of sleep/wake states. Deficiency of orexin signaling results in the sleep disorder narcolepsy-cataplexy in humans, dogs, and rodents. These findings have brought about the possibility of novel therapies for sleep disorders including narcolepsy-cataplexy. Furthermore, accumulating evidence has indicated that the orexi...

متن کامل

Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.

Orexins are peptides produced by lateral hypothalamic neurons that exert a prominent role in the maintenance of wakefulness by activating orexin-1 (OX1R) and orexin-2 (OX2R) receptor located in wake-active structures. Pharmacological blockade of both receptors by the dual OX1/2R antagonist (2R)-2-[(1S)-6,7-dimethoxy-1-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydroisoquinolin-2(1H)-yl]-N-methy...

متن کامل

Kinetic properties of “dual” orexin receptor antagonists at OX1R and OX2R orexin receptors

Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in clinical settings and thorough investigations of pharmacokinetics and pharmacodynamics can predict contributing factors such as duration of action and undesirable effects. To this end, we studied the interactions between various "dual" orex...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: IUPHAR/BPS guide to pharmacology CITE

سال: 2023

ISSN: ['2633-1020']

DOI: https://doi.org/10.2218/gtopdb/f51/2023.1