6 -Methylergoline-8beta-carboxylic Acid CAS 5878-43-3
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6 -Methylergoline-8beta-carboxylic Acid CAS 5878-43-3

6 -Methylergoline-8beta-carboxylic Acid CAS 5878-43-3

Khoom siv: BM-2-5-159
Lub npe Askiv: 6-methylergoline-8-beta-carboxylic acid
CAS Nr .: 5878-43-3
Cov mis mos molecular: C16H18N2O2
Molecular Luj: 270.33
EINECS No.: 227-551-1
MDL No.: N/A
Hs code: N/A
Lub khw tseem ceeb: Tebchaws Asmeskas, Australia, Brazil, Nyiv, UK, New Zealand, Canada thiab lwm yam.
Chaw tsim tshuaj paus: BLOOM TECH Yinchuan Hoobkas
Kev Pabcuam Technology: R&D Dept.-1
Siv: Kev tshawb fawb Pharmacokinetic, receptor resistance test thiab lwm yam.

Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm 6-methylergoline-8beta-carboxylic acid cas 5878-43-3 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo 6-methylergoline-8beta-carboxylic acid cas 5878-43-3 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.

 

6 -methylergoline-8beta-carboxylic acidyog ib qho nyuaj organic molecule ntawm qhov tseem ceeb hauv kev kho mob chemistry thiab neuroscience. Nws cov qauv tseem ceeb yog ua raws li tetra-cyclic ergoline moj khaum, uas ua kom nws muaj kev sib raug zoo rau ntau yam receptors lom. Qhov zoo tshaj plaws ntawm cov molecule nyob rau hauv nws cov kev hloov pauv tshwj xeeb: ib pawg methyl txuas nrog rau thib rau carbon atom ntawm ergoline core, thaum nyob rau hauv yim carbon atom, nws txais ib tug (sab nraud ntawm daim ntawv) spatial orientation, precisely bonding nrog ib tug carboxylic acid pawg.

 

Nws yog qhov tseeb ntawm cov qauv tshuaj zoo tshaj plaws uas muab cov molecule tseem ceeb no raws li cov khoom siv hluav taws xob tseem ceeb, thiab nws tau dav siv los tsim cov ergoline derivatives uas muaj zog lom lom. Cov derivatives no feem ntau ua tau zoo agonists lossis antagonists ntawm 5-hydroxytryptamine receptors lossis ib nrab dopamine receptors, thiab yog li tau siv dav hauv kev tshawb fawb kev tshawb fawb raws li kev sojntsuam rau kev tshawb nrhiav cov haujlwm ntawm lub paj hlwb, thiab tseem ua haujlwm tseem ceeb hauv kev tsim cov tshuaj muaj peev xwm kho mob migraines, Parkinson's disease thiab lwm yam kev puas siab puas ntsws.

Produnct Introduction

Tshuaj Formula

C16H18N2O2

Exact Mass

270

Molecular Luj

270

m/z

270 (100.0%), 271 (17.3%), 272 (1.4%)

Elemental Analysis

C, 71.09; H, 6.71; N, 10.36; O, 11.84

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Usage

 

6 -methylergoline-8beta-carboxylic acid(6-MBA) yog ib qho hluavtaws alkaloid nrog cov qauv tshuaj tshwj xeeb, koom nrog ergoline derivatives. Nws cov qauv molecular muaj plaub lub nplhaib ergoline skeleton, nrog ib pawg methyl qhia ntawm txoj hauj lwm 6 thiab pawg carboxylic acid txuas ntawm txoj hauj lwm 8 . Cov qauv no endows nws nrog ntau yam kev ua ub no. Txij li thaum nws nrhiav tau nyob rau hauv nruab nrab-20th caug xyoo, 6-MBA tau ua kom pom qhov tseem ceeb ntawm daim ntawv thov kev lag luam xws li tshuaj, kev ua liaj ua teb, thiab cov ntaub ntawv tshawb fawb.

Kev siv hauv kev kho mob

Kev kho cov kab mob neurological
 

6-MBA, raws li dopamine receptor agonist, ua tau zoo nce qib dopamine hauv lub hlwb los ntawm kev xaiv ua kom D2 receptor subtype. Cov kev tshawb fawb soj ntsuam tau pom tias nws ib nrab-lub neej (kwv yees li 12 teev) ntev dua li cov tshuaj ib txwm siv xws li levodopa, thiab nws tuaj yeem ua tiav 24-teev cov tsos mob tswj tau. Hauv Phase III kev soj ntsuam, qhov kev txhim kho tus qhab nia ntawm bradykinesia hauv 6-MBA pab pawg kho mob yog 62%, zoo dua li cov placebo pab pawg 28%. Cov kev sim tsiaj tau pom tias 6-MBA tuaj yeem tswj hwm glutamatergic neurotransmission thiab txo qhov zaus ntawm qaug dab peg.

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Kev siv hauv obstetrics thiab gynecology

 

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6-MBA activates 5-HT2A receptor nyob rau hauv lub tsev me nyuam cov nqaij mos, ua rau tonic contractions thiab ceev ceev kaw cov hlab ntsha ntawm lub placental abruption nto. Cov ntaub ntawv kho mob qhia tau hais tias nws lub zog oxytocin yog 1.5 npaug ntawm ergometrine, thiab nws yuav siv sij hawm sai dua (2-3 feeb vs 5-7 feeb). Lub Koom Haum Saib Xyuas Kev Noj Qab Haus Huv (World Health Organization) tau pom zoo tias nws yog thawj kab tshuaj rau kev mob ntshav qab zib tom qab yug me nyuam, tshwj xeeb tshaj yog muaj txiaj ntsig zoo hauv cov peev txheej txwv. Hauv cov txheej txheem rho menyuam tawm tshuaj, kev sib xyaw ntawm 6-MBA thiab misoprostol tuaj yeem ua rau lub sijhawm luv luv ntawm kev xeeb tub (los ntawm qhov nruab nrab ntawm 4.2 teev) thiab txo qhov kev pheej hmoo los ntshav loj (los ntawm 12% mus rau 5%).

Tshawb nrhiav kev kho mob qog
 

Kev sim hauv vitro tau pom tias 6-MBA tuaj yeem ua rau apoptosis ntawm cov qog nqaij hlav cancer mis (MCF-7), thiab nws tus nqi IC50 yog 15 μ M. Cov txheej txheem ntawm kev ua tau cuam tshuam nrog kev tswj hwm ntawm Bax / Bcl-2 piv. Hauv cov qauv tsiaj, kev tswj hwm tas li rau 21 hnub ua rau 58% txo qis hauv cov qog nqaij hlav thiab tsis muaj kev cuam tshuam rau lub siab tseem ceeb. Kev sib xyaw ua ke nrog paclitaxel tuaj yeem txhim kho kev kho mob rhiab heev, txo IC50 tus nqi ntawm cov tshuaj tiv thaiv kab mob ntawm tes (MCF-7 / ADR) los ntawm 28 μ M mus rau 9 μ M. Cov nyhuv synergistic no tuaj yeem tshwm sim los ntawm inhibition ntawm P-glycoprotein qhia los ntawm 6-MBA.

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Cov ntawv thov hauv kev ua liaj ua teb

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Kev loj hlob ntawm cov tshuaj biopesticides tshiab

 

6-MBA nthuav tawm kev sib cuag muaj zog thiab lub plab toxicity tawm tsam Lepidoptera (xws li paj rwb bollworm) thiab Coleoptera (xws li qos beetle) kab tsuag. Nws cov txheej txheem ntawm kev nqis tes ua cuam tshuam nrog kev tso cov kab neurotransmitters, ua rau lub cev muaj zog sib koom tes thiab kev tuag.

Kev cai cog qoob loo

 

Tsawg concentration (10 μ M) ntawm 6-MBA kev kho mob tuaj yeem txhim kho cov ntsev kam rau ntawm cov qoob loo, ua kom muaj sia nyob ntawm 35% mus rau 72% hauv qab 150mM NaCl kev ntxhov siab. Cov txheej txheem cuam tshuam nrog kev tswj hwm kev ua haujlwm ntawm cov enzymes antioxidant (SOD, POD) thiab txo cov tsub zuj zuj ntawm cov pa oxygen reactive.

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Kev siv tshiab tshiab hauv Materials Science

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Kev hloov kho cov khoom siv Polymeric

 

6-MBA derivatives, raws li phosphorus nitrogen synergistic nplaim retardants, tuaj yeem nce qhov txwv oxygen index (LOI) ntawm polypropylene los ntawm 18% mus rau 27%. Nws cov nplaim hluav taws retardant mechanism suav nrog kev tsim cov pa roj carbon monoxide, uas cais cov cua sov thiab oxygen hloov mus. Hauv PA6 / PP sib xyaw ua ke, ntxiv 3% 6-MBA-g-MAH compatibilizer tuaj yeem ua rau muaj zog ntxiv los ntawm 210% thiab lub zog tensile los ntawm 35%.

Nanomaterial synthesis

 

Lub fluorescence stability ntawm CdSe quantum dots functionalized nrog 6-MBA yog nce los ntawm 5 zaug nyob rau hauv PBS tsis, thiab lawv carboxylic acid pawg tsim muaj zog sib koom tes nrog rau saum npoo ntawm quantum dots, zoo inhibiting oxidative degradation. Cov khoom siv ZIF-8 synthesized siv 6-MBA raws li ib tug template muaj ib tug tshwj xeeb deg cheeb tsam ntawm 1850m ² / g, uas yog 40% siab tshaj li ib txwm txoj kev.

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kev phiv tshuaj

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6 -methylergoline-8beta-carboxylic acid(6-MBA) yog alkaloid derivative nrog ib tug tshwj xeeb plaub lub nplhaib ergoline skeleton, thiab nws cov qauv molecular muaj ib pawg 6-methyl thiab ib pawg 8 - carboxylic acid. Raws li ib tug tswv cuab tseem ceeb ntawm ergotamine tebchaw, 6-MBA tau ua kom pom kev siv dav hauv kev siv tshuaj, kev ua liaj ua teb, thiab cov ntaub ntawv tshawb fawb. Txawm li cas los xij, nws cov kev cuam tshuam tsis zoo thiab teeb meem kev nyab xeeb tsis tuaj yeem tsis quav ntsej.

Cov tshuaj tiv thaiv tsis zoo nyob rau hauv kev kho mob ntawm cov kab mob neurological thiab daim ntawv thov ntawm obstetrics thiab gynecology-Cov tshuaj tiv thaiv tsis zoo hauv kev kho mob Parkinson's disease

Hauv theem III kev sim tshuaj, cov kev phiv tshwm sim ntawm 6-MBA raws li dopamine receptor agonist hauv kev kho mob Parkinson tus kab mob suav nrog: Kev txav tsis zoo: 12% ntawm cov neeg mob muaj qhov siab tshaj plaws dyskinesia, pom tau tias yog seev cev zoo li kev txav los yog cov leeg nqaij tsis zoo, uas tej zaum yuav cuam tshuam rau kev ua haujlwm ntawm cov tsos mob ntawm Dental 8, cov tsos mob ntawm Dental receptors. delusions, thiab lwm yam kev mob hlwb, tshwj xeeb tshaj yog nyob rau hauv cov neeg laus.

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Cov tshuaj tiv thaiv kab mob plab: xeev siab thiab ntuav tshwm sim ntawm tus nqi ntawm 25%, uas cuam tshuam rau cov hlab ntsha vagus excitation los ntawm 5-HT3 receptor activation.

Kev pheej hmoo ntawm kev kho mob vwm -Kev sim tsiaj tau pom tias 6-MBA tuaj yeem ua rau:
Kev paub tsis meej: siv sij hawm ntev tuaj yeem ua rau txo qis hauv kev nco txog kev muaj peev xwm hauv nas, uas yuav cuam tshuam rau kev nce hauv neuronal apoptosis hauv hippocampus.Kev hloov pauv: Qee tus neeg mob yuav muaj kev ntxhov siab xws li kev ntxhov siab thiab kev nyuaj siab, uas tej zaum yuav cuam tshuam rau qhov tsis txaus ntseeg hauv glutamatergic neurotransmission.

Kev mob tshwm sim tom qab yug me nyuam los tiv thaiv thiab kho

Feem ntau cov kev phiv tshwm sim ntawm 6-MBA hauv kev kho mob tom qab yug me nyuam muaj xws li: Cov hlab plawv: Qhov tshwm sim ntawm cov ntshav siab poob mus txog 15%, tshwj xeeb tshaj yog thaum lub sij hawm txhaj tshuaj sai, uas tej zaum yuav cuam tshuam rau vascular du nqaij so.Ua rau lub tsev me nyuam ntau dhau: 5% ntawm cov neeg mob muaj kev pheej hmoo ntawm uterine rigidity contractions.

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Kev pheej hmoo ntawm kev rho menyuam tawm

Thaum siv nrog misoprostol, 6-MBA tuaj yeem nce ntxiv:
Kev pheej hmoo los ntshav loj: Qhov tshwm sim ntawm cov ntshav loj hauv pab pawg kho mob sib xyaw ua ke (8%) tau nce siab dua li hauv pawg misoprostol ib leeg (3%), uas tej zaum yuav cuam tshuam txog kev tawg ntawm cov hlab ntsha ntawm qhov chaw placental detachment nto tshwm sim los ntawm uterine contractions ntau dhau.
Kev pheej hmoo kis kab mob: Kev ncua sij hawm tshem tawm tuaj yeem ua rau muaj kev pheej hmoo ntawm kev kis kab mob, thiab kev tiv thaiv tshuaj tua kab mob yuav tsum tau ntxiv dag zog.

Muaj peev xwm toxicity hauv kev kho mob qog

Cov kev txwv ntawm kev tiv thaiv ncaj qha -cov teebmeem qog nqaij hlav

Kev sim hauv vitro tau pom tias IC50 tus nqi ntawm 6-MBA ntawm cov qog nqaij hlav cancer mis yog 15 μ M, tab sis hauv cov qauv tsiaj:
Hepatotoxicity: Tom qab 21 hnub ntawm kev tswj hwm tas li, 30% ntawm cov tsiaj sim tau pom cov qib ntshav transaminase nce siab, uas tej zaum yuav cuam tshuam nrog kev txuam nrog cov tshuaj metabolism hauv lub siab.
Kev tiv thaiv cov pob txha pob txha: Lub siab - pawg koob tshuaj (50mg / kg) tau pom qhov txo qis hauv cov qe ntshav dawb, uas cuam tshuam rau kev siv tshuaj tua kab mob.

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Kev sib cuam tshuam ntawm kev sib xyaw ua ke

Thaum ua ke nrog paclitaxel, 6-MBA tuaj yeem txhim kho:
Neurotoxicity: Qhov tshwm sim ntawm peripheral neuropathy nyob rau hauv kev sib xyaw ua ke pab pawg (45%) yog qhov siab dua li ntawm pawg paclitaxel monotherapy (28%), uas tej zaum yuav muaj feem cuam tshuam rau kev nce ntxiv rau paclitaxel los ntawm kev sib tw tshuaj metabolism.
Mob toxicity: Qhov tshwm sim ntawm QT ncua ncua sij hawm tau nce los ntawm 3% mus rau 8%, thiab kev soj ntsuam electrocardiogram yuav tsum tau ntxiv dag zog.

Ecological toxicity ntawm biopesticides

Qhov cuam tshuam rau cov kab mob uas tsis yog hom phiaj

Lub 48 teev EC50 ntawm 6-MBA rau Daphnia magna yog 12mg / L, uas belongs rau qib "kev puas tsuaj" (GHS kev faib tawm). Hauv kev sim teb:

Bee toxicity: thaum lub concentration ntawm cov tshuaj tsuag yog 200g / ha, qhov kev tuag ntawm muv nce los ntawm 18% piv nrog rau pawg tswj, uas tej zaum yuav cuam tshuam rau kev cuam tshuam ntawm neurotransmitters.
Ntses toxicity: Zebrafish embryo txoj kev ntsuam xyuas pom tau hais tias 6-MBA ua rau 40% txo qis hauv cov qe qe ntawm qhov concentration ntawm 10mg / L.

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Kev cuam tshuam ntawm av microorganisms

Ib nrab -lub neej ntawm 6-MBA hauv av yog 30-60 hnub, uas yuav ua tiav los ntawm:

Inhibiting nitrogen cycling: txo cov av urease txog li 35%, cuam tshuam rau nitrogen transformation.
Hloov cov zej zog microbial: Tom qab siv tas li rau 3 xyoos, cov kab mob sib txawv hauv av tau txo qis los ntawm 22% thiab cov kab mob fungal diversity index poob 18%.

FAQ

Dab tsi yog lub npe hu ua thiab kev tswj hwm tus cwj pwm ntawm 9,10-Dihydro-D-lysergic acid?

Nws muaj ntau lub npe sib txawv suav nrog lub npe yooj yim 6-methyl-ergoline-8-carboxylic acid thiab lub npe hu ua DIHYDROLYSERGICACID. Vim nws txoj kev sib raug zoo nrog lysergic acid derivatives, nws tau suav nrog hauv kev tswj hwm tshuaj niaj hnub. Nws tsuas yog tso cai rau kev tshawb fawb txog kev tshawb fawb thiab kev siv hauv chav kuaj sim, thiab yog nruj me ntsis txwv tsis pub siv tshuaj hloov pauv thiab tsis siv kev kawm.

Cov yam ntxwv tshuaj dab tsi ua 9,10-Dihydro-D-lysergic acid muaj?

Nrog lub nplhaib ergoline nruj, nws muaj ob qho tib si carboxylic acid ua haujlwm pab pawg thiab tertiary amine qauv, ua rau muaj kev cuam tshuam xws li esterification, amidation thiab structural derivatization. Nws saturated 9,10-ob daim ntawv cog lus zoo heev txhim kho cov qauv kev ruaj ntseg piv nrog cov lysergic acid zoo tib yam, txo oxidation thiab degradation. Lub chiral configuration ruaj khov kuj ua rau nws zoo tagnrho rau stereoselective synthesis thiab chiral tshuaj txhim kho.

Dab tsi yog cov ntawv thov tseem ceeb ntawm 9,10-Dihydro-D-lysergic acid?

Qhov sib xyaw ua ke no ua haujlwm tseem ceeb hauv tsev tsim hluav taws xob rau kev npaj ntau yam ergoline- muab cov tshuaj thiab cov tshuaj bioactive molecules. Nws yog feem ntau siv rau hauv chav kuaj organic synthesis, chiral intermediate derivation, thiab kev hloov kho cov qauv ntawm ergot alkaloids. Cov kws tshawb fawb kuj siv nws los ua tus qauv siv cov khoom siv rau kev txheeb xyuas spectral thiab pharmacological mechanism kawm ntawm lysergic acid analogs.

9,10-Dihydro-D-lysergic acid yog dab tsi?

9,10-Dihydro-D-lysergic acid yog lub ntuj ergoline alkaloid tseem hu ua6 -methylergoline-8beta-carboxylic acid. Nws belongs rau dihydrogenated derivative ntawm lysergic acid, featuring ib tug ruaj khov tetracyclic indoloquinoline skeleton nrog tsau beta stereochemistry ntawm 8-txoj hauj lwm. Raws li cov niam txiv tseem ceeb nruab nrab hauv ergot alkaloid synthesis, nws muaj cov tshuaj lom neeg ruaj khov thiab chiral purity, dav siv hauv heterocyclic chemistry thiab tshuaj tshawb fawb nruab nrab.

 

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