
nalphuraphine

nalphuraphine (inn, yousen) (brand paeru remitch; maajee abhivruddhi sankethaalu truck-820, esi-820, enti-9938) anedi oka antipruritic (yanti-itch drugg), idhi hemodialysis cheyinchukuntunna deerghakaalika moothrapindaala vyaadhi unna vyaktulalo euramic pruritus chikitsa kosam japaanlo vikrayinchabadutundi. idhi κ-opioid grahakanni (core) sakriyam chestundi mariyu saktivantamainadi, empika cheyabadinadi mariyu kendramgaa churukuga untundi. idhi clinical upayogam kosam aamodinchabadina modatidi, mariyu prastutam empika chesina ekaika kaar agonist. dheenini charitralo "mottamodati naan-narcotic opioid drugg" gaa kooda anumanaspadamga suuchistaaru.
charitra.
nalphuraphine opioid virodhi nultrexone yokka nirmaanaatmaka maarpu nundi udbhavinchindi. idhi mottamodata 1998loe samslaeshanha cheyabadindi mariyu vargeekarinchabadindi, mariyu japaanlo 2009loe brand paeru remitch kinda intravenous aushadhamgaa clinical upayogam kosam aamodinchabadindi. nalphuraphine developer kooda airopalo brand paeru winfuran kinda aamodam pondaadu, conny marketing authorization applicationnu european medicines agency tiraskarinchindi. eee aushadham modata shastrachikitsalo analgesicga abhivruddhi cheyabadindi, conny nociseption yokka janthu namoonaalalo prabhaavavantamgaa unnappatikee, maanavulalo upasamana prabhaavaala yokka spashtamgaa aamodayogyam kaani sambhavam kaaranamgaa takkuva chikitsa motaadulalo idhi antipruriticga tirigi uddesinchabadindi. 2015 natiki, deerghakaalika kaaleya vyaadhi unna rogulaku japaanlo collustatic pruritus chikitsa kosam mariyu united stateslo euramic pruritus chikitsa kosam kooda nalphuraphine clinical trialslo undhi.
prabhavalu.
itara kaar agonistula maadirigaa kakunda, nalphuraphine maanavulalo halucinogenic prabhavalanu utpatti cheyadu. 30 microgramla varaku unna oke intramuscular injectionlanu maanavulu baga thattukogalaru, ayithe 40 microgramla motaadu "mitamaina pravartanaa/manasika dushprabhaavaalanu" utpatti chestundi (bahusha upasamanaanni suuchistumdi), ayithe spashtamgaa etuvanti psychotamimatic ledhaa diasphoric prabhavalanu utpatti cheyaledu. elukalalo, takkuva motaadu nalphuraphine (10-40 μg/kilolu) conditioned plays preference ledhaa verrini utpatti cheyaledani kanugonabadindi, ayithe adhika motaadu (80 microlu/kilolu) gananeeyamaina plays verrini prerepinchindi. clinical trialslo kanipinche takkuva motaadu nalfurafin yokka atyanta saadhaarana dushprabhaavamgaa nidralemi (rogulalo 10-15% loe gamaninchabadindi), konni itara pratikuula prabhavalu gamaninchabaddaayi. adanamgaa, oka samvatsaram paatu eee aushadhaanni teesukunna rogulaku chikitsa chesina tarvaata nalfurafin yokka antipruritic prabhaavaalaku sahanam kanugonabadaledu, mariyu nalfurafin maanavulalo saareerakamgaa ledhaa maanasikamgaa aadhaarapadataaniki etuvanti aadharalu choopinchaledu. itara kaar agonistulaku sambandhinchi jantuvulalo analgesia mariyu sedation vanti prabhaavaalaku eee aushadham takkuva sahanam choopistundi. jantuvulalo, nalfurafine anty-scratch, antinosyseptive, sedative mariyu mootravisarjana prabhavalanu utpatti chestundi.
charya yokka yantraangam.
nalphuraphine anedi κ-opioid receptor (core) (kii = 75 pm; isi50 = 25 pm) yokka noti dwara churukaina, kendramgaa panichese, atyanta saktivantamaina, empika chesina puurti agonist. paina cheppinatlugaa, itara aushadhaalaku sambandhinchi kaar agonistga nalphuraphine asaadhaarana lakshanaalanu chooputundi. mukhyamgaa, idhi elukalalo prototypical core agonist yuu-50488kii puurtigaa pratyaamnaayam kaadu, idhi rendu sammelanaala vivakshata prabhavalalo gunaatmaka vyatyaasaalanu suuchistumdi. antekakunda, yuu-50488 maadirigaa kakunda, idhi elukalalo conditioned plays verri ledhaa praadhaanyatanu utpatti cheyadu. eee aushadham 4,5-epoximorphinon utpannam, mariyu itara kaar agonistulaku sambandhinchi nirmanatmakamga pratyekamainadi. nalphuraphine anedi core yokka pakshapaata agonist ledhaa core upa-rakam-selective agonist kaavacchu. vaastavaaniki, idhi core yokka pakshapaata agonistga panichestundani kanugonabadindi, β-arrestine signalling "inn vitronu" sakriyam cheyadaaniki ishtapadutundi, conny viruddhamgaa, β-arrestine core agonist-prerita virakti kii baadhyata vahistundi, mariyu nalfurafine daani "inn vitronu" profile thoo sthiramgaa laeni "inn vivonu" viruddhamaina prabhavalanu chooputundi. anduvalla, eee aushadham yokka vibhina vidhanalu mariyu prabhavalanu spashtam cheyadaaniki marinta parisoedhana avasaram.
alfurafine anedi micro-opioid graahakamtho bandhinchadaaniki mariyu eee pradaesamloe balaheenamaina pakshika agonist karyakalapalanu kaligi undataaniki "inn vitro" gaa kanugonabadindi, ayithe korku sambandhinchi chaalaa takkuva anubandham kaligi untundi. ayithe, "inn vivo" loe, nalphuraphine jantuvulu ledhaa maanavulalo morr agonism ledhaa satrutvam yokka suuchanalu choopinchaledu, veetilo pratiphalinche ledhaa balapariche prabhavalu ledhaa saareeraka aadhaarapadataaniki etuvanti aadharalu laevu.
parisoedhana.
maadakadravyaala durviniyogam, vyasanam mariyu aadhaarapadataaniki sambandhinchina vividha rakaala janthu namoonaalalo nalphuraphine prabhaavavantamgaa unnatlu kanugonabadindi mariyu eee vyaadhulaku kotta sambhaavya chikitsanu suuchimchavachchu. elukalalo, eee aushadham kokain yokka vivakshata mariyu bahumati prabhavalanu mariyu marphin yokka bahumati mariyu locomotor prabhavalanu taggistundi mariyu nikotin upasamharana yokka mcamillamine-precipited pratikuula prabhavanni taggistundi.