Muscarine (muscarinum)
Qhov no yog ib qho ntawm feem ntau lom alkaloids, uas tau pom los ntawm Schmideberg. Nws tau pom nyob rau hauv yoov agaric Amanita muscaria los yog Agaricus Muscarius L. Los ntawm lub subfamily ntawm agaric tsev neeg Hymenomycetes (Hymenomycetes). Kuj muscarine tau pom nyob rau hauv fungi Boletus luridus thiab Amanita pantherina thiab nyob rau hauv fungus Inocybe.
lub zog
Qhov no nceb-derived alkaloid yog hu ua nceb los yog ntuj muscarine, thiab nws cov mis empirical yog C5H15NO8, thaum tsis pom cov qauv qauv. Ntuj muscarine yog odorless thiab tasteless thiab yog ib tug syrupy kua nrog ib tug muaj zog alkaline cov tshuaj tiv thaiv, uas, thaum qhuav nyob rau hauv lub xub ntiag ntawm sulfuric acid, maj mam hloov mus rau hauv lub xeev crystalline. Nyob rau hauv huab cua, alkaloid crystals kis tau sai heev, thiab muscarine rov qab mus rau ib tug syrupy kua. Nws yog soluble heev hauv cawv thiab dej, tsis zoo nyob rau hauv chloroform, thiab tag nrho insoluble hauv ether. Yog tias nws tau kub siab tshaj 100 degrees, ces nws raug rhuav tshem, thiab tsis hnov tsw tsw ntawm luam yeeb tshwm. Thaum kho nrog txhuas oxide los yog caustic alkali thiab rhuab, nws hloov mus rau hauv trimethylamine, thiab nrog sulfuric los yog hydrochloric acid nws tsim crystalline ntsev. Muaj qhov kev xav tias cov qauv ntawm muscarine zoo ib yam li cov qauv ntawm choline (C5H15NO2):
H3C / CH2CH (OH) 2
H3C — N
H3C / OH
Tab sis qhov kev sim ntawm Schmiedeberg thiab Harnack qhia tau hais tias cov khoom siv alkaloid, tau txais los ntawm choline, cuam tshuam rau tsiaj txawv dua li lub ntuj. Cov kev sim no tau pom tias cov khoom siv dag zog thiab cov muscarines tsis zoo ib yam.
Qhov tseem ceeb rau tshuaj
Ob qho tib si lub ntuj nceb alkaloid thiab cov khoom siv hluavtaws tsis yog tam sim no siv rau kev kho mob, tab sis lawv qhov tseem ceeb ntawm kev kho mob siab heev. Thaum yav tas los, kev sim tau ua los kho mob vwm thiab cov txheej txheem oncological ntawm cov qog nrog muscarine. Nws kuj tau npaj los siv rau hauv cov kab mob qhov muag thiab kev kho mob ntawm ulcers. Tab sis tag nrho cov kev sim no tau nres vim qhov tshwj xeeb toxicity ntawm cov compound.
Tab sis muscarine muaj tshuaj lom, theoretical thiab pharmacological tseem ceeb. Nws belongs rau parasympathicotropic pab pawg neeg ntawm cov tshuaj lom, uas muaj ib tug stimulating nyhuv ntawm peripheral parasympathicotropic qab haus huv, thaum lub alkaloid muaj ib tug nruj me ntsis xaiv ntawm lub paj hlwb. Cov yam ntxwv no ua rau nws muaj txiaj ntsig zoo li tus neeg sawv cev tshuaj uas tuaj yeem siv rau hauv kev sim xws li hluav taws xob stimulation lossis hloov nws.
Yog hais tias nyob rau hauv me me koob tshuaj koj qhia natural muscarine mus rau hauv lub cev ntawm ib tug tsiaj, ces muaj ib tug slowdown nyob rau hauv lub plawv kev ua si (tsis zoo inotropic thiab chronotropic teebmeem), thiab nyob rau hauv loj koob nws thawj ua rau ib tug qeeb thiab tsis muaj zog ntawm systolic contractions. Thiab tom qab ntawd hauv theem diastolic, tag nrho lub plawv nres tshwm sim.
Kev ua ntawm lub cev
Cov kev tshawb fawb los ntawm ntau tus kws tshawb fawb pom tau tias muscarine muaj qhov ua rau tuag tes tuag taw ntawm lub paj hlwb peripheral ntawm txoj hlab ntsws, ua rau muaj kev sib zog ntxiv ntawm cov leeg ntawm lub plab thiab cov hnyuv, thiab kev txav ntawm cov hnyuv pom txawm tias los ntawm cov kab mob hauv plab. . Yog hais tias muscarine yog siv nyob rau hauv ib koob loj, ces muaj erratic peristaltic txav, uas yog hloov los ntawm antiperistalsis, ntuav thiab raws plab pib. Ib qho kev qhia meej ntawm kev lom muscarine yog qhov mob ntawm qhov contractions ntawm tag nrho lub plab lossis nws tus kheej ntu, ua raws li kev so. Raws li Schmideberg, muscarine muaj zog heev rau cov hnyuv thiab plab, tsis tsuas yog vim nws cov nyhuv ntawm qhov kawg ntawm lub vagus qab haus huv uas nyob rau hauv cov kab mob no, tab sis kuj vim nws cov nyhuv ntawm ganglion hlwb ntawm Auerbach plexus. . Tsis tas li ntawd, cov alkaloid no ua rau muaj kev sib kis ntawm lwm cov leeg nqaij, piv txwv li, hauv tsev menyuam, tus po thiab zais zis. Kev cog lus tshwm sim los ntawm qhov ua rau muaj kev cuam tshuam ntawm cov tshuaj ntawm cov peripheral receptors ntawm cov hlab ntsha parasympathetic nyob rau hauv cov kabmob no, nrog rau cov txiaj ntsig ntawm kev cuam tshuam ntawm cov hlab ntsha tsis siv neeg ganglion, los ntawm kev sib piv nrog nws tshwm sim li cas hauv lub cev. plawv. Cov menyuam kawm ntawv ntawm lub qhov muag nyob rau hauv tus ntawm muscarine yog heev nqaim, ib tug spasm ntawm kev pab tsim. Ob qhov tshwm sim no yog vim qhov kev ua ntawm alkaloid ntawm cov receptors ntawm parasympathetic fibers ntawm lub paj hlwb oculomotor nyob rau hauv cov hlab ntsha ncig ntawm lub iris thiab hauv cov leeg ciliary.
Schmideberg pom tias nceb muscarine tsis ua rau lub cev nqaij daim tawv, tsis zoo li cov muscarine dag, uas ua rau lub cev tsis muaj zog. Qhov no tom qab tau lees paub los ntawm Hans Meyer thiab Gonda. Yog li, curare-zoo li cov khoom yog tshwj xeeb rau hluavtaws muscarine muab los ntawm choline.
Muscarine nceb activates cov qog ntawm lub plab zom mov, stimulates lub secretion ntawm cov kua tsib thiab pancreatic kua txiv. Nws kuj ua rau kom salivation, tawm hws thiab lacrimation. Kev tso zis ntawm qaub ncaug nyob rau hauv qhov kev txiav txim ntawm muscarine yog piav qhia los ntawm qhov tseeb tias nws irritates peripheral paj hlwb xaus (qhov no tau ua pov thawj los ntawm Schmideberg). Kev tso tawm ntawm tag nrho lwm cov qog yog txhim kho los ntawm kev ua kom khaus ntawm muscarine ntawm lawv cov hlab ntsha scapular. Hauv qhov no, lub hom phiaj ntawm kev ua muscarine yog cov paj hlwb peripheral.
Tus antagonist ncaj qha ntawm muscarine yog atropine, uas thaiv cov nyhuv ntawm muscarine los ntawm kev tuag tes tuag taw ntawm cov hlab ntsha parasympathetic. Qhov no yog tshwm sim nyob rau hauv cov ntaub ntawv uas muscarine muaj ib tug irritating nyhuv ntawm peripheral receptors ntawm ib qho ntawm cov hlab ntsha parasympathetic. Yog li ntawd, atropine sai sai tshem tawm cov diastolic plawv nres thiab qeeb ntawm lub plawv dhia provoked los ntawm muscarine. Atropine tseem txwv tsis pub muaj peristalsis, antiperistalsis thiab spasms ntawm lub plab thiab cov hnyuv, kev pab cuam spasm thiab cov menyuam kawm ntawv contraction, zais zis contraction, nrog rau muaj zog secretory muaj nuj nqi ntawm ntau yam qog (hws, salivary thiab lwm yam). Atropine sulphate exerts nws antagonistic nyhuv ntawm muscarine nyob rau hauv ib tug me me npaum li cas (0,001-0,1 mg). Muscarine kuj tseem paub tias yuav tsum txwv qhov kev txiav txim ntawm atropine ntawm Qav lub plawv, qhov muag, caj pas submandibular, thiab hws qog. Yog li ntawd, muaj kev xav tias muscarine thiab atropine yog kev sib nrig sib antagonists. Tab sis nyob rau tib lub sijhawm, ntau muscarine yuav tsum tau (txog 7 g) thiaj li yuav tsum tau txiav txim siab ntawm atropine. Hauv qhov no, nws tsis yog qhov tsim nyog los hais tias muscarine muaj kev cuam tshuam tshwj xeeb rau atropine, thiab ntau tus kws kho mob tau xav tias qhov teeb meem ntawm ob sab antagonism ntawm ob lub tebchaw tseem tsis tau daws.
Tsis tas li ntawd, muscarine antagonists muaj xws li aconitine, hyoscyamine, veratrin, scopolamine, physostigmine, digitalin, delphinium, camphor, helleborine, chloral hydrate, adrenaline. Muaj cov lus tseeb nthuav qhia los ntawm Tsondek tias calcium chloride kuj muaj cov nyhuv antagonistic rau muscarine.
Qhov rhiab heev ntawm cov tsiaj sib txawv rau muscarine tuaj yeem sib txawv heev. Yog li ntawd, tus miv tuag los ntawm kev txhaj tshuaj subcutaneous ntawm muscarine ntawm koob tshuaj 4 mg tom qab ob peb teev, thiab ntawm koob tshuaj 12 mg tom qab 10-15 feeb. Cov dev tso siab rau cov tshuaj alkaloid ntau dua. Tib neeg yog rhiab heev rau cov khoom no. Schmideberg thiab Koppe tau ua qhov kev sim ntawm lawv tus kheej thiab pom tias kev txhaj tshuaj muscarine ntawm koob tshuaj 3 mg twb ua rau muaj tshuaj lom, uas yog tshwm sim los ntawm salivation muaj zog heev, maj ntshav mus rau lub taub hau, kiv taub hau, tsis muaj zog, liab ntawm daim tawv nqaij, xeev siab thiab ntse. mob hauv plab, tachycardia, tsis pom kev tsis pom kev thiab spasm ntawm kev pab. Kuj tseem muaj hws ntau ntxiv ntawm lub ntsej muag thiab me ntsis tsawg dua ntawm lwm qhov ntawm lub cev.
Daim duab ntawm kev lom
Nyob rau hauv cov ntaub ntawv ntawm fungus lom, daim duab yuav zoo ib yam li cov lus piav qhia ntawm muscarine lom, tab sis feem ntau nws tseem txawv vim hais tias ya agaric muaj ntau yam tshuaj lom atropine-zoo li tshuaj thiab lwm yam tebchaw uas, ntawm ib sab, muaj feem xyuam rau lub hauv paus. paj hlwb, thiab ntawm qhov tod tes, nres qhov kev txiav txim ntawm muscarine. Yog li ntawd, kev ua xua tuaj yeem tshwm sim los ntawm cov tsos mob ntawm lub plab thiab cov hnyuv (xws li xeev siab, ntuav, mob, raws plab) lossis cov tsos mob sib txawv, piv txwv li, lub xeev ntawm intoxication nrog delirium thiab muaj zog excitement, kiv taub hau, irresistible siab xav ua kom puas txhua yam. nyob ib ncig ntawm, qhov yuav tsum tau txav mus. Tom qab ntawd trembling tshwm sim thoob plaws hauv lub cev, epileptiform thiab tetanic convulsions tshwm sim, cov menyuam kawm ntawv nthuav dav, cov mem tes nrawm nrawm dua, ua tsis taus pa cuam tshuam, ua tsis zoo, lub cev kub poob qis thiab lub xeev ntawm lub cev qhuav dej. Hauv qhov xwm txheej no, kev tuag tshwm sim hauv ob lossis peb hnub. Nyob rau hauv cov ntaub ntawv ntawm rov qab, ib tug neeg rov qab tau qeeb heev, lub xeev ntawm hyperleukocytosis yog pom nyob rau hauv cov ntshav, thiab cov ntshav nws tus kheej coagulates tsis zoo heev. Tab sis txog niaj hnub no, tsis muaj cov ntaub ntawv ntseeg tau thiab lees paub tag nrho ntawm cov ntshav hloov, ib yam li tsis muaj cov ntaub ntawv ntawm kev hloov pauv pathological thaum muaj tshuaj lom.
Thawj pab
Ua ntej ntawm tag nrho cov, nyob rau hauv cov ntaub ntawv ntawm lom nrog nceb, nws yog tsim nyog los tshem tawm cov ntsiab lus ntawm lub plab thiab cov hnyuv. Ua li no, siv emetics, gastric lavage nrog kev sojntsuam, thiab cov hnyuv nrog ib qho enema. Hauv cov koob tshuaj loj lawv haus cov roj castor. Yog hais tias cov tsos mob ntawm kev lom cov yam ntxwv ntawm muscarine predominate, ces atropine yog txhaj subcutaneously. Yog tias kev lom neeg tshwm sim feem ntau nyob rau hauv kev cuam tshuam ntawm cov tshuaj zoo li atropine, ces atropine tsis tuaj yeem siv los ua tshuaj tua kab mob.
Artificial muscarine, uas yog muab los ntawm choline, yog qhov feem ntau kawm. Tsawg heev tsis paub txog lwm cov muscarines dag. Anhydromuscarine tsub kom qhov tso tawm hws thiab qaub ncaug, thiab tsis cuam tshuam rau lub qhov muag thiab lub plawv. Nws ua rau tuag vim ua pa tuag tes tuag taw. Isomuscarine tsis ua rau lub plawv nres, tab sis ua rau lub plawv dhia qeeb, uas tuaj yeem thim rov qab nrog atropine. Nyob rau hauv cov noog, nws ua rau ib tug contraction ntawm cov menyuam kawm ntawv, thiab nyob rau hauv cov tsiaj nws muaj ib tug curare-zoo li cov nyhuv ntawm lub cev muaj zog paj hlwb thiab txhim khu lub secretory muaj nuj nqi ntawm cov qog, tsis cuam tshuam rau lub qhov muag thiab cov hnyuv, tab sis ua rau kom ntshav siab. Ptomatomuscarine muaj cov nyhuv zoo sib xws rau cholinemuscarine, uas qhia tias lawv muaj cov qauv tshuaj zoo sib xws. Cov tshuaj pharmacological ntawm uromuscarins tseem tsis tau kawm. Tib yam tuaj yeem hais txog cov tshuaj pharmacological ntawm carnomoscarin.