Umkhiqizi wempuphu ye-Agomelatine Inombolo ye-CAS: 138112-76-2 Ubumsulwa obungu-99% okungenani bezithako ezengeziwe
Ividiyo Yomkhiqizo
Amapharamitha Omkhiqizo
| Igama lomkhiqizo | I-Agomelatine |
| Elinye igama | I-N-[2-(7-Methoxy-1-naphthyl)ethyl]acetamide;I-N-[2-(7methoxynaphthalen-1-yl)ethyl]acetamide |
| Inombolo ye-CAS | 138112-76-2 |
| Ifomula yama-molecule | C15H17NO2 |
| Isisindo sama-molecule | 243.3082 |
| Ubumsulwa | 99.0% |
| Ukubukeka | Impuphu emhlophe |
| Ukupakisha | 1kg/isikhwama 25kg/isigubhu |
| Isicelo | Izinto zokusetshenziswa zomkhiqizo wezempilo |
Isingeniso somkhiqizo
I-Agomelatine yaqala ukwethulwa eYurophu ngo-2009 futhi manje isivunyelwe ukusetshenziswa emazweni angaphezu kuka-70. Ngokungafani nemithi yokucindezeleka yendabuko, i-agomelatine isebenza ngokugxila kuma-melatonin nama-serotonin receptors ebuchosheni. Ngokusebenza njenge-agonist kuma-receptor e-melatonin, i-agomelatine isiza ekulungiseni amaphethini okulala aphazamisekile avame ukuhlotshaniswa nokucindezeleka. Le ndlela ayisizi nje kuphela ukuthuthukisa ikhwalithi yokulala kodwa futhi isiza ekubuyiseleni imigqi yemvelo ye-circadian. Ngaphezu kwalokho, i-agomelatine isebenza njengomphikisi kuma-receptor athile e-serotonin (ama-receptor angu-5-HT2C). Lesi senzo esiyingqayizivele esiphindwe kabili sithuthukisa ngokungaqondile ukutholakala kwe-serotonin ebuchosheni, i-neurotransmitter ephethe ukulawula isimo sengqondo. Ngokulawula amazinga e-serotonin, i-agomelatine ingasebenza njengomphilisi wokucindezeleka ophumelelayo, iqeda izimpawu ezifana nokudabuka, ukulahlekelwa isithakazelo, imizwa yecala noma ukungabi nalutho. Ngaphezu kwalokho, i-agomelatine inganikeza ezinye izinzuzo. Ucwaningo luphakamisa ukuthi ingasiza ekuthuthukiseni ukusebenza kwengqondo Ucwaningo lubonisa amandla ayo okuthuthukisa inkumbulo, ukunaka, kanye nomsebenzi wokuphatha, okwenza kube yindawo ejabulisayo yocwaningo lwesikhathi esizayo.
Isici
(1) Ubumsulwa obuphezulu: I-Agomelatine ingathola imikhiqizo yobumsulwa obuphezulu ngezinqubo zokukhiqiza zokucwenga. Ubumsulwa obuphezulu busho ukutholakala okungcono kwe-bioavailability kanye nokusabela okuncane okubi.
(2) Ukuphepha: Ukuphepha okuphezulu, ukusabela okungekuhle okumbalwa.
(3) Ukuzinza: I-Agomelatine inokuqina okuhle futhi ingagcina umsebenzi wayo kanye nomphumela ngaphansi kwezimo ezahlukene zokugcinwa.
Izicelo
I-Agomelatine iyisidakamizwa sokucindezeleka kanye ne-melatonin antagonist. Inciphisa izimpawu zokucindezeleka ngokulawula ama-receptor e-melatonin MT1 (kunciphisa izimpawu ze-cortical alarm) kanye nama-receptor e-MT2 (isigqi sokulala se-circadian) kanye namazinga e-serotonin. Ithathwa ebusuku, ilingisa isigqi semvelo sokukhululwa kwe-melatonin futhi ingathuthukisa kakhulu ikhwalithi yokulala. Indlela esebenza ngayo iphula ohlelweni lwendabuko lokudlulisa i-monoamine. Ivuselela ama-receptor e-melatonin MT1 kanye ne-MT2 futhi iphikisana nama-receptor e-5-HT2C. Ithuthukisa ikhwalithi yokulala, ibuyisela isigqi sebhayoloji, futhi inomphumela wokucindezeleka; phakathi kwazo, ngokulwa nama-receptor e-5-HT2C kulwelwesi lwe-postsynaptic, ingakhulisa ukukhishwa kwe-DA kanye ne-NE ku-prefrontal cortex, isebenzise umphumela wokucindezeleka. Lapho i-MT agonism kanye nokuphikisana kwama-receptor e-5-HT2C kuhlangana, umphumela oyingqayizivele wokubambisana ungakhiqizwa, ukhuthaze ukukhishwa kwe-DA kanye ne-NE eyengeziwe endaweni yobuchopho ye-PFC, ukuqinisa umphumela wokucindezeleka. Ngaphezu kwalokho, i-agomelatine ingakhuthaza ukukhishwa kwe-neurotrophic factor etholakala ebuchosheni ku-PFC futhi ivimbele ukukhishwa kwe-glutamate okubangelwa ukucindezeleka endaweni yobuchopho ye-amygdala.
