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Orexin B (mouse)

Endogenous agonist at OX1 and OX2 CAS# 202801-92-1

Orexin B (mouse)

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Chemical structure

Orexin B (mouse)

3D structure

Chemical Properties of Orexin B (mouse)

Cas No. 202801-92-1 SDF Download SDF
PubChem ID 90479795 Appearance Powder
Formula C126H215N45O34S M.Wt 2936.43
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 1 mg/ml in water
Sequence RPGPPGLQGRLQRLLQANGNHAAGILTM

(Modifications: Met-28 = C-terminal amide)

SMILES CCC(C)C(C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCSC)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(C)NC(=O)C(CC1=CNC=N1)NC(=O)C(CC(=O)N)NC(=O)CNC(=O)C(CC(=O)N)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(CCC(=O)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C2CCCN2C(=O)C3CCCN3C(=O)CNC(=O)C4CCCN4C(=O)C(CCCNC(=N)N)N
Standard InChIKey RLVZFBVFVIDDPQ-GWQFQBPDSA-N
Standard InChI InChI=1S/C126H215N45O34S/c1-18-65(12)99(120(202)166-82(49-64(10)11)117(199)168-100(69(16)172)121(203)156-72(101(133)183)37-44-206-17)167-97(181)57-144-102(184)66(13)150-103(185)67(14)152-111(193)83(50-70-53-140-59-149-70)165-116(198)85(52-93(132)177)155-95(179)55-146-106(188)84(51-92(131)176)161-104(186)68(15)151-107(189)76(32-35-90(129)174)159-114(196)80(47-62(6)7)164-115(197)81(48-63(8)9)163-109(191)74(27-21-40-143-126(138)139)157-110(192)77(33-36-91(130)175)160-113(195)79(46-61(4)5)162-108(190)73(26-20-39-142-125(136)137)153-94(178)54-145-105(187)75(31-34-89(128)173)158-112(194)78(45-60(2)3)154-96(180)56-147-118(200)87-29-23-43-171(87)123(205)88-30-24-41-169(88)98(182)58-148-119(201)86-28-22-42-170(86)122(204)71(127)25-19-38-141-124(134)135/h53,59-69,71-88,99-100,172H,18-52,54-58,127H2,1-17H3,(H2,128,173)(H2,129,174)(H2,130,175)(H2,131,176)(H2,132,177)(H2,133,183)(H,140,149)(H,144,184)(H,145,187)(H,146,188)(H,147,200)(H,148,201)(H,150,185)(H,151,189)(H,152,193)(H,153,178)(H,154,180)(H,155,179)(H,156,203)(H,157,192)(H,158,194)(H,159,196)(H,160,195)(H,161,186)(H,162,190)(H,163,191)(H,164,197)(H,165,198)(H,166,202)(H,167,181)(H,168,199)(H4,134,135,141)(H4,136,137,142)(H4,138,139,143)/t65-,66-,67-,68-,69+,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,99-,100-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Orexin B (mouse)

DescriptionEndogenous agonist at orexin receptors. May be involved in the regulation of feeding, sleep-wake cycle and other hypothalamic functions.

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References on Orexin B (mouse)

GABA(B) receptor-mediated modulation of hypocretin/orexin neurones in mouse hypothalamus.[Pubmed:16627567]

J Physiol. 2006 Jul 15;574(Pt 2):399-414.

Hypocretin/orexin (Hcrt) is a critical neurotransmitter for the maintenance of wakefulness and has been implicated in several other functions, including energy metabolism and reward. Using whole-cell patch-clamp recordings from transgenic mice in which enhanced green fluorescent protein was linked to the Hcrt promoter, we investigated GABAergic control of the Hcrt neurones in hypothalamic slices. Bath application of GABA or muscimol caused an early hyperpolarization mediated by Cl(-) and a late depolarization mediated by the efflux of bicarbonate. These GABA(A) receptor-mediated responses were blocked by picrotoxin and bicuculline. Under the GABA(A) blockade condition, GABA produced consistent hyperpolarization, decreased firing rate and input resistance. The selective GABA(B) agonist (R)-baclofen caused a similar response with an EC(50) of 7.1 mum. The effects of (R)-baclofen were blocked by the GABA(B) antagonist CGP 52432 but persisted in the presence of tetrodotoxin, suggesting direct postsynaptic effects. The existence of GABA(B) modulation was supported by GABA(B(1)) subunit immunoreactivity on Hcrt cells colabelled with antisera to the Hcrt-2 peptide. Furthermore, GABA(B) receptor activation inhibited the presynaptic release of both glutamate and GABA. (R)-Baclofen depressed the amplitude of evoked excitatory postsynaptic currents (EPSCs) and inhibitory synaptic currents (IPSCs), and also decreased the frequency of both spontaneous and miniature EPSCs and IPSCs with a modest effect on their amplitudes. These data suggest that GABA(B) receptors modulate Hcrt neuronal activity via both pre- and postsynaptic mechanisms, which may underlie the promotion of non-rapid eye movement sleep and have implications for the use of GABA(B) agonists in the treatment of substance addiction through direct interaction with the Hcrt system.

Induction of outward current by orexin-B in mouse peritoneal macrophages.[Pubmed:9862423]

FEBS Lett. 1998 Nov 27;440(1-2):51-4.

To define effects of novel feeding regulating peptides, orexins, in immunocompetent cells, ion channel activity in mouse peritoneal macrophages was analyzed by the perforated patch-clamp method. Orexin-B (OX-B) induced an outward current at smaller holding potentials than K+ equilibrium potentials. Reversal potentials of OX-B induced current were dependent on external K+ concentrations but not on external Cl- concentration. Orexin-A is less effective than OX-B. Quinine blocked the outward current and tetraethylammonium partially suppressed the current. These results suggest that OX-B can modulate macrophage functions through the activation of Ca2+-dependent K2+ channels.

The hypocretin/orexin ligand-receptor system: implications for sleep and sleep disorders.[Pubmed:10906799]

Trends Neurosci. 2000 Aug;23(8):359-65.

The molecules originally described as the hypocretins and subsequently as the orexins were initially implicated in the control of food intake. Recent observations implicate this newly-described neurotransmitter system in the sleep disorder narcolepsy and, potentially, in the regulation of normal sleep processes. This article reviews the research that led to the isolation of the hypocretin/orexin peptides, their receptors and the activity of these molecules as we currently understand them. A model is proposed in which the cells that make these peptides might be involved in arousal state control.

Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.[Pubmed:9491897]

Cell. 1998 Feb 20;92(4):573-85.

The hypothalamus plays a central role in the integrated control of feeding and energy homeostasis. We have identified two novel neuropeptides, both derived from the same precursor by proteolytic processing, that bind and activate two closely related (previously) orphan G protein-coupled receptors. These peptides, termed orexin-A and -B, have no significant structural similarities to known families of regulatory peptides. prepro-orexin mRNA and immunoreactive orexin-A are localized in neurons within and around the lateral and posterior hypothalamus in the adult rat brain. When administered centrally to rats, these peptides stimulate food consumption. prepro-orexin mRNA level is up-regulated upon fasting, suggesting a physiological role for the peptides as mediators in the central feedback mechanism that regulates feeding behavior.

Description

Orexin B, rat, mouse is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.

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