IPSU - CAS 1373765-19-5
Category: Inhibitor
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Molecular Formula:
C23H27N5O2
Molecular Weight:
405.49
COA:
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Targets:
Orexin Receptor (OX Receptor)
Description:
IPSU is a selective, orally available and brain penetrant OX2 receptor antagonist (pKi= 7.85) with 6-fold selectivity over OX1 receptors.
Brife Description:
A selective OX2 receptor antagonist
Synonyms:
2-(1H-indol-3-ylmethyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one
Solubility:
DMSO: ≥ 30 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
702.0±70.0 ℃ at 760 Torr
Density:
1.32±0.1 g/cm3
InChIKey:
PCMHOSYCWRRHTG-UHFFFAOYSA-N
InChI:
1S/C23H27N5O2/c1-30-20-7-11-24-22(26-20)27-13-9-23(10-14-27)8-4-12-28(21(23)29)16-17-15-25-19-6-3-2-5-18(17)19/h2-3,5-7,11,15,25H,4,8-10,12-14,16H2,1H3
Canonical SMILES:
COC1=NC(=NC=C1)N2CCC3(CCCN(C3=O)CC4=CNC5=CC=CC=C54)CC2
1.Distinct effects of IPSU and suvorexant on mouse sleep architecture.
Hoyer D;Dürst T;Fendt M;Jacobson LH;Betschart C;Hintermann S;Behnke D;Cotesta S;Laue G;Ofner S;Legangneux E;Gee CE Front Neurosci. 2013 Dec 10;7:235. doi: 10.3389/fnins.2013.00235. eCollection 2013.
Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, SB-649868, suvorexant (MK-4305), and filorexant (MK-6096), have shown promise for the treatment of insomnias and sleep disorders. Whether antagonism of both OX1R and OX2R is necessary for sleep induction has been a matter of some debate. Experiments using knockout mice suggest that it may be sufficient to antagonize only OX2R. The recent identification of an orally bioavailable, brain penetrant OX2R preferring antagonist 2-((1H-Indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one (IPSU) has allowed us to test whether selective antagonism of OX2R may also be a viable strategy for induction of sleep. We previously demonstrated that IPSU and suvorexant increase sleep when dosed during the mouse active phase (lights off); IPSU inducing sleep primarily by increasing NREM sleep, suvorexant primarily by increasing REM sleep. Here, our goal was to determine whether suvorexant and IPSU affect sleep architecture independently of overall sleep induction. We therefore tested suvorexant (25 mg/kg) and IPSU (50 mg/kg) in mice during the inactive phase (lights on) when sleep is naturally more prevalent and when orexin levels are normally low.
2.Impact of pelvic floor muscle training on sexual function of women with urinary incontinence and a comparison of electrical stimulation versus standard treatment (IPSU trial): a randomised controlled trial.
Jha S;Walters SJ;Bortolami O;Dixon S;Alshreef A Physiotherapy. 2018 Mar;104(1):91-97. doi: 10.1016/j.physio.2017.06.003. Epub 2017 Jun 23.
AIMS: ;To evaluate the clinical and cost-effectiveness of electric stimulation plus standard pelvic floor muscle training compared to standard pelvic floor muscle training alone in women with urinary incontinence and sexual dysfunction.;METHODS: ;Single centre two arm parallel group randomised controlled trial conducted in a Teaching hospital in England. Participants were women presenting with urinary incontinence and sexual dysfunction. The interventions compared were electric stimulation versus standard pelvic floor muscle training.;OUTCOME MEASURES: ;included Prolapse and Incontinence Sexual function Questionnaire (PISQ) physical function dimension at post-treatment (primary); other dimensions of PISQ, SF-36; EQ-5D, EPAQ, resource use, adverse events and cost-effectiveness (secondary outcomes).;RESULTS: ;114 women were randomised (Intervention n=57; Control group n=57). 64/114 (56%).;PARTICIPANTS: ;had valid primary outcome data at follow-up (Intervention 30; Control 34). The mean PISQ-PF dimension scores at follow-up were 33.1 (SD 5.5) and 32.3 (SD 5.2) for the Intervention and Control groups respectively; with the Control group having a higher (better) score. After adjusting for baseline score, BMI, menopausal status, time from randomisation and baseline oxford scale score the mean difference was -1.
3.Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors.
Callander GE;Olorunda M;Monna D;Schuepbach E;Langenegger D;Betschart C;Hintermann S;Behnke D;Cotesta S;Fendt M;Laue G;Ofner S;Briard E;Gee CE;Jacobson LH;Hoyer D Front Neurosci. 2013 Dec 3;7:230. doi: 10.3389/fnins.2013.00230. eCollection 2013.
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" orexin receptor antagonists and the orexin receptors, OX1R and OX2R, over time using saturation and competition radioligand binding with [(3)H]-BBAC ((S)-N-([1,1'-biphenyl]-2-yl)-1-(2-((1-methyl-1H-benzo[d]imidazol-2-yl)thio)acetyl)pyrrolidine-2-carboxamide). In addition, the kinetics of these compounds were investigated in cells expressing human, mouse and rat OX1R and OX2R using FLIPR® assays for calcium accumulation. We demonstrate that almorexant reaches equilibrium very slowly at OX2R, whereas SB-649868, suvorexant, and filorexant may take hours to reach steady state at both orexin receptors. By contrast, compounds such as BBAC or the selective OX2R antagonist IPSU ((2-((1H-Indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one) bind rapidly and reach equilibrium very quickly in binding and/or functional assays.
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CAS 1373765-19-5 IPSU

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