(Ala11, D-Leu15)-Orexin B human RSGPPGLQGRAQRL-(D-Leu)-QASGNHAAGILTM-amide
Description
Application Data
Description
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Highly potent and selective OX2 receptor agonist
Application Data
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Data Sheet Material Safety Data Sheet (MSDS)Catalogue number crb1000496 Molecular Weight 898.5 Sequence (one letter code) RSGPPGLQGRAQRL-(D-Leu)-QASGNHAAGILTM-amide Sequence (three letter code) H-Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Ala-Gln-Arg-Leu-(D-Leu)-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2 Molecular Weight 898.5 Purity >95% Storage -20°C References Asahi et al., (2003). Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B. Bioorg. Med. Chem. Lett. 13(1) 111. PMID: 12467628
Shahid et al., (2012). Orexin A in rat rostral ventrolateral medulla is pressor, sympatho-excitatory, increases barosensitivity and attenuates the somato-sympathetic reflex. Br. J. Pharmacol. 165(7) 2292. PMID: 21951179
Wang et al., (2018). The Orexin/Receptor System: Molecular Mechanism and Therapeutic Potential for Neurological Diseases. Front. Mol. Neurosci. 11. PMID: 30002617
Orexin B is one of two closely related peptides; the orexins (also known as hypocretins). These small neuropeptides are secreted from orexin-containing neurons, located mainly in the lateral hypothalamus (LH). Orexins function via the binding and activation of two G-protein–coupled receptors (GPCRs); orexin receptor type 1 (OX1) and 2 (OX2).
[Ala(11), D-Leu(15)]orexin-B is a highly potent and selectiveOX2 receptor agonist which can discriminate between the OX1 and OX2 receptors, with a 400-fold selectivity for the OX2 over OX1. [Ala(11), D-Leu(15)]orexin-B is therefore a beneficial tool for addressing the functional roles of OX2.
The L-leucine residue at position 11 of orexin B is important for selectivity to OX2 over OX1. L-Alanine substitution at position 11 and D-leucine substitution at positions 15 maintain the potency of orexin-B to OX2, while significantly reducing the potency for OX1.
Orexins play several vital roles in a range of physiological activities, including: circadian rhythm; feeding behaviour; energy balance; glucose metabolism; neuroendocrine functions; stress-adaptive responses and reward and addiction. Orexins have also been linked to the pathological processes of neurological diseases such as: narcolepsy; depression; ischemic stroke; drug addiction and Alzheimer’s disease.