Qhov sib txawv tseem ceeb ntawm kev thim rov qab agonist thiab antagonist yog qhov kev hloov pauv agonist khi rau tib lub receptor zoo li tus agonist tab sis ua rau cov lus teb rov qab rau tus agonist thaum tus antagonist khi rau ib qho receptor uas yuav cuam tshuam kev cuam tshuam thiab Kev ua haujlwm ntawm ob qho tib si agonist thiab inverse agonist ntawm receptor.
Receptors yog macromolecules koom nrog hauv cov tshuaj lom neeg hauv thiab nruab nrab ntawm cov hlwb. Cov receptors ncaj qha lossis ncaj qha tswj cov txheej txheem ntawm cov txheej txheem biochemical los ntawm kev khi rau cov ligands lossis tshuaj. Inverse agonist thiab antagonist yog ob hom tshuaj uas cuam tshuam nrog receptors sib txawv.
Dab tsi yog Inverse Agonist?
Ib tus agonist inverse yog ib yam tshuaj uas khi rau tib lub receptor raws li tus agonist tab sis coj los ntawm cov lus teb rov qab rau tus agonist. Yuav tsum muaj qhov yuav tsum tau ua ua ntej rau qhov kev hloov pauv agonist ntawm ib qho receptor tshwj xeeb. Hauv lwm lo lus, tus receptor yuav tsum muaj kev sib koom ua ke ntawm kev ua haujlwm yam tsis muaj ligand. Tus agonist augments qhov kev ua ntawm ib qho receptor tshwj xeeb tshaj nws qib basal. Tus agonist inverse txo cov kev ua ntawm ib tug receptor hauv qab theem basal.
ABAA, muopioid, histamine, melanocortin, thiab beta-adrenergic receptors muaj peculiar inverse agonists. Piv txwv li, GABAA receptor muaj ib qho agonist xws li muscimol uas tsim cov nyhuv relaxant whereas, tus inverse agonist rau GABAA receptor xws li Ro15-4513. tsim kom muaj kev ntxhov siab. Qee cov beta-carbolines kuj yog inverse agonists rau GABAA receptors uas tsim convulsive thiab anxiogenic teebmeem.
Daim duab 01: Qhov Zoo Tshaj Plaws Cov Lus Teb Kov
Ob tus paub zoo endogenous inverse agonists yog agouti-txog peptide (AgRP) thiab nws cuam tshuam peptide agouti signaling peptide (ASIP) uas khi rau tib neeg melanocortin receptors 4 thiab 1 (Mc4R thiab Mc1R) nrog me me. kev sib raug zoo. Tus agonist rau cov receptor no yog cov tshuaj hormone α-MSH. AgRP inhibits melanocortin-receptor signaling. Cov receptors no txuas ncaj qha rau cov metabolism thiab tswj lub cev hnyav. AgRP ua rau cov receptor kom qab los noj mov thiab txo cov metabolism thiab siv zog. Ntxiv mus, naloxone thiab n altrexone cov tshuaj kuj ua raws li ib feem ntawm cov agonists ntawm mu-opioid receptors. Yuav luag txhua cov tshuaj tiv thaiv kab mob yog cov agonists inverse uas ua haujlwm ntawm H1 receptors thiab H2 receptors.
Tus neeg ntxeev siab yog dab tsi?
Tus antagonist yog ib yam tshuaj uas khi rau lub receptor uas yuav cuam tshuam kev cuam tshuam thiab kev ua haujlwm ntawm ob qho tib si agonist thiab inverse agonist ntawm receptor. Cov tshuaj antagonist tuaj yeem cuam tshuam nrog kev ua haujlwm ntawm receptor proteins. Lawv qee zaum hu ua blockers xws li alpha-blockers, beta-blockers, thiab calcium channel blockers.
Daim duab 02: Agonist vs Antagonist
Cov antagonists ntxias lawv cov teebmeem los ntawm kev khi rau lub vev xaib nquag lossis lwm qhov chaw allosteric ntawm lub receptor. Cov kev ua ntawm antagonists yuav thim rov qab los yog irreversible. Feem ntau cov antagonists yog cov antagonists thim rov qab. Lawv yuav khi thiab unbind ib receptor ntawm tus nqi txiav txim los ntawm receptor-ligand kinetics. Ntawm qhov tod tes, irreversible antagonists covalently khi rau lub hom phiaj receptor. Lawv tsis tuaj yeem raug tshem tawm; Phenoxybenzamine yog ib qho piv txwv zoo ntawm ib qho irreversible antagonist (alpha-blocker). Nws ruaj khov rau α adrenergic receptors thiab tiv thaiv kev khi ntawm adrenaline thiab noradrenaline. Tsis tas li ntawd, cov antagonists tau muab faib ua ntau hom raws li lawv cov txheej txheem: kev sib tw antagonists, tsis sib tw antagonists, tsis sib tw antagonists, thiab ntsiag to antagonists.
Dab tsi yog qhov zoo sib xws ntawm Inverse Agonist thiab Antagonist?
- Ob leeg yog siv hauv tshuaj ua tshuaj.
- Lawv ob leeg khi rau receptors.
- Ob leeg tuaj yeem khi rau qhov chaw nquag ntawm tus neeg txais kev pab.
- Qhov cuam tshuam ntawm ob leeg yog tawm tsam agonists.
Qhov txawv ntawm Inverse Agonist thiab Antagonist yog dab tsi?
Ib tus agonist inverse yog ib yam tshuaj uas khi rau tib lub receptor raws li tus agonist tab sis coj los ntawm cov lus teb rov qab rau ntawm tus agonist thaum tus antagonist yog ib yam tshuaj uas khi rau ib qho receptor uas yuav cuam tshuam kev cuam tshuam thiab kev ua haujlwm. ntawm ob qho tib si agonist thiab inverse agonist ntawm tus receptor. Yog li, qhov no yog qhov sib txawv tseem ceeb ntawm kev sib hloov agonist thiab antagonist. Tsis tas li ntawd, inverse agonist tsuas yog khi rau cov receptors uas muaj kev sib koom ua ke ntawm kev ua haujlwm. Nyob rau hauv sib piv, antagonist khi rau ob hom receptors uas muaj ib theem ntawm kev ua si thiab ligand-induced kev ua si.
Cov infographic hauv qab no nthuav tawm qhov sib txawv ntawm qhov sib txawv ntawm cov agonist thiab antagonist hauv daim ntawv teev npe.
Summary – Inverse Agonist vs Antagonist
Hauv biochemistry thiab pharmacology, receptors yog cov qauv tshuaj uas muaj cov proteins. Lawv tau txais thiab hloov cov cim qhia uas tuaj yeem ua ke rau hauv cov kab ke lom neeg xws li cov hlwb. Cov txheej txheem biochemical ntawm tes yog ncaj qha lossis ncaj qha tswj hwm los ntawm cov receptors tshwj xeeb. Inverse agonists thiab antagonists yog ob hom tshuaj uas cuam tshuam nrog receptors sib txawv. Ib qho kev sib hloov agonist khi rau tib lub receptor raws li tus agonist tab sis coj los ntawm cov lus teb rov qab rau tus agonist. Ntawm qhov tod tes, tus antagonist khi rau lub receptor uas yuav cuam tshuam kev cuam tshuam thiab kev ua haujlwm ntawm ob qho tib si agonist thiab inverse agonist ntawm receptor. Yog li, qhov no yog cov ntsiab lus ntawm qhov sib txawv ntawm kev sib hloov agonist thiab antagonist.
