Ingcaciso yeMveliso
Rimonabant powder ividiyo
I-Raw Rimonabant powder esisiseko Iimpawu
| igama: | I-Rimonabant Powder (SR141716) |
| CAS: | 168273-06-1 |
| I-molecular Formula: | C22H21Cl3N4O |
| Isisindo somzimba: | 463.8 |
| Melt Point: | Ngama-230 ° C - 240 ° C |
| Isitoreji sokugcina: | Umgubo -20 ° C 3 iminyaka |
| umbala: | Umgubo omhlophe-grey |
Imvelaphi yeRimonabant
Imvelaphi yembali ye-Rimonabant ibuyele ekupheleni kwe-1990 kunye ne-2000 yokuqala xa abaphandi baqala ukuphanda inkqubo ye-endocannabinoid kunye nefuthe layo elinokubakho kwiinkqubo ezahlukeneyo ze-physiological, kubandakanywa ukulawulwa kokutya kunye nokulinganisela kwamandla.
Ngeli xesha, izazinzulu zichonge ii-cannabinoid receptors emzimbeni, ezaziwa ngokuba zii-CB1 receptors, ezifumaneka kakhulu kwingqondo kunye nezicubu ze-peripheral.
Ukukhuthazwa kukuqonda okukhulayo kwenkqubo ye-endocannabinoid yokubandakanyeka ekulawuleni ukutya, iinkampani zamachiza ziqalise ukuphuhliswa kwe-CB1 ekhethiweyo ye-receptor antagonists ukujolisa ukutyeba kunye neemeko ezinxulumene nazo.
Kwi-1999, inkampani yaseFransi yamachiza i-Sanofi-Synthélabo (ngoku eyi-Sanofi) yaqala ukuphuhlisa iyeza elibizwa ngokuba yi-Rimonabant.Rimonabant yenzelwe ukuthintela ngokufanelekileyo i-CB1 receptors, ngokufanelekileyo ukuvimbela umsebenzi we-endocannabinoid system.
Izilingo zeklinikhi zenziwa ukuvavanya ukusebenza kunye nokukhuseleka kweRimonabant ekulawuleni ukukhuluphala kunye nokuphazamiseka kwe-metabolic ehambelanayo.Izifundo zibonise iziphumo ezithembisayo, ezibonisa ukulahleka kwesisindo kunye nokuphuculwa kwezinto ezinobungozi benhliziyo, njengamanqanaba e-cholesterol kunye nokuxhatshazwa kwe-insulin.
Ngokusekelwe kwiziphumo ezilungileyo ezivela kwezi zilingo, i-Rimonabant ifumene imvume yokulawula kwi-2006 kwi-European Union phantsi kwegama lokuthengisa i-Acomplia.Yayiyiyeza lokuqala elaphuhliswa ngokukodwa ukunyangwa kokukhuluphala kwiminyaka elishumi.
Nangona kunjalo, nangona ukuphumelela kwayo kokuqala, iRimonabant ijongene nemingeni kunye neengxabano. amazwe amaninzi, kubandakanywa iManyano yaseYurophu ngo-2008.
Ukuhoxiswa kweRimonabant kubonise ukubaluleka kokuvavanya ngononophelo ukhuseleko kunye neengozi zengqondo ezinxulumene neziyobisi ezijoliswe kwinkqubo ye-endocannabinoid.Ngelixa i-Rimonabant ayizange izalisekise isithembiso sayo sokuqala njengeyeza lokuchasana nokukhuluphala, linikeze ukuqonda okubalulekileyo kwi-complex interplay phakathi kwe-endocannabinoid. inkqubo kunye nolawulo lwe-metabolic.
Ukususela ekuhoxisweni kweRimonabant, iinzame zophando ziye zaqhubeka zihlola amandla onyango ekujoliseni inkqubo ye-endocannabinoid, kodwa kugxininise ngakumbi ekuphuhliseni iikhompawundi ezinciphisa iingozi zengqondo ezinxulumene ne-CB1 receptor blockade.
I-Rimonabant Powder
I-Rimonabant Powder yinto yonyango eyafumana ingqalelo ekusetyenzisweni kwayo kwinkalo yonyango.Ivela kwiklasi yamachiza eyaziwa ngokuba yi-selective cannabinoid receptor antagonists.I-Rimonabant yaqalwa yaphuhliswa njengeyeza lokuchasana nokutyeba, ijolise kwinkqubo ye-endocannabinoid yokunceda ukulawula. ukutya kunye nobunzima.
Ifom yePowder yeRimonabant ivumela ukuphatha lula kunye nokusabalalisa ngexesha leenkqubo zokuqulunqa.I-Rimonabant Powder iyancibilika ngokukhawuleza emanzini, oko kuthetha ukuba ine-solubility elinganiselweyo kwiisombululo ezinamanzi.Nangona kunjalo, inokubonisa ukunyibilika okungcono kwi-solvents eziphilayo ezifana ne-ethanol, i-methanol, okanye Ipropylene glycol.Iimpawu ze-solubility zeRimonabant zibalulekile ingqalelo ngexesha lokuphuhliswa kokuqulunqwa.
Indlela yesenzo yeRimonabant
Indlela yokusebenza ye-Rimonabant ibandakanya ukusebenzisana kwayo kunye nenkqubo ye-endocannabinoid emzimbeni.I-Rimonabant yinto ekhethiweyo ye-cannabinoid receptor antagonist, ngokuyinhloko ijolise kwi-receptors ye-CB1 efunyenwe kwingqondo kunye nezicubu ze-peripheral.
Xa idliwe, iRimonabant ibophelela kwaye ivimba i-CB1 receptors, ikhusela ukusebenza kwezi receptor ngama-cannabinoids angapheliyo afana ne-anandamide.Ngokuthintela i-CB1 receptors, iRimonabant imodareyitha umsebenzi wenkqubo ye-endocannabinoid, edlala indima kwiinkqubo ezahlukeneyo ze-physiological, kubandakanywa nomdla wokutya. ukulawulwa, ibhalansi yamandla, kunye ne-lipid metabolism.
Ngokukodwa, ukuvalwa kwe-CB1 receptors nguRimonabant kuchaphazela oku kulandelayo:
Ukulawula ukutya
I-CB1 i-receptors ibandakanyeka ekulawuleni ukutya kunye nokutya.Xa i-receptors ye-CB1 ivuliwe, ivuselela ukukhululwa kwee-neuropeptides ezibangela indlala kunye nokwandisa iipropati ezivuzayo zokutya.I-Rimonabant's blockade ye-CB1 receptors iyanciphisa umsebenzi we-endocannabinoid system, ekhokelayo. ukunciphisa ukutya kunye nokunciphisa ukutya.
Inkcitho yamandla
Inkqubo ye-endocannabinoid ichaphazela inkcitho yamandla ngokulawula i-thermogenesis, inkqubo apho umzimba uvelisa ukushisa kunye nokutshisa iikhalori.Ngokuthintela i-CB1 receptors, i-Rimonabant inokukhuthaza ukwanda kwenkcitho yamandla, igalelo ekulahlekeni kwesisindo.
I-Lipid Metabolism
I-CB1 receptor activation ihambelana nokunyuka kwe-lipogenesis (ukugcinwa kwamafutha) kunye nokunciphisa i-lipolysis (ukuchithwa kwamafutha) .I-Rimonabant's antagonism ye-CB1 receptors inokubangela ukunyanzeliswa kwe-lipogenesis kunye nokukhuthazwa kwe-lipolysis, enokuthi iholele ekunciphiseni ukuqokelela kwamafutha omzimba.
Kubalulekile ukuba uqaphele ukuba ngelixa i-Rimonabant ngokuyinhloko yenza njenge-CB1 i-receptor antagonist, inokuphinda ibonise ezinye iziphumo ezongezelelweyo okanye intsebenziswano kunye nezinye i-receptors okanye iinkqubo emzimbeni. uphando.
Indlela yokusebenza ye-Rimonabant Powder iyafana neyoRimonabant kwezinye iifom.I-Rimonabant Powder ibhekisela kwifom ye-Powdered ye-Rimonabant yeziyobisi, eyona nto ikhethiweyo ye-cannabinoid receptor antagonist.
Xa i-Rimonabant Powder ilawulwa, mhlawumbi ngomlomo okanye ngokuqulunqwa kwiifom ezahlukeneyo ze-dosage, ifumana ukuchithwa kunye nokufunxa emzimbeni.Xa ifunyenwe, isebenzisana ne-endocannabinoid inkqubo ngokujolisa kwi-receptors ye-CB1 efunyenwe kwingqondo kunye nezicubu ze-peripheral.
Ziziphi iimpembelelo zeRimonabant?
I-Rimonabant, iyeza elichasayo lokutyeba, yaqala yaphuhliswa ukunceda abantu abanengxaki yokulawula ubunzima. Inzuzo yayo ephambili yayikukwazi ukucinezela ukutya kunye nokukhuthaza ukwehla kobunzima.
Ukunciphisa Ukutya
I-Rimonabant yenzelwe ukunciphisa ukutya kunye nokukhuthaza ukulahlekelwa kwesisindo ngokuthintela i-CB1 receptors kwingqondo ebandakanyekayo ekulawuleni ukutya.
Ukuhla ukusinda
Njengomphumo wokunciphisa ukutya, i-Rimonabant yayilindeleke ukuba iholele ekulahlekeni kwesisindo kubantu abanokukhuluphala okanye ukutyeba.Izilingo zeklinikhi zibonise ukuba unyango lweRimonabant lunokubangela ukunciphisa ubunzima obuninzi xa kudibaniswa nokutya okulawulwayo kunye nokuzivocavoca.
Uphuculo lweMetabolic
I-Rimonabant ibonise iinzuzo ezinokuthi ziphucule iiparitha ze-metabolic ezinxulumene nokukhuluphala, ezifana neeprofayili ze-lipid, ukunyanzeliswa kwe-insulin, kunye namanqaku omngcipheko we-cardiovascular risk.
Uncedo lokuyeka ukutshaya
I-Rimonabant iphandwe ngokusetyenziswa kwayo njengoncedo ekuyekeni ukutshaya.Kwakucingelwa ukuba ngokuthintela i-CB1 receptors, i-Rimonabant inokunciphisa i-nicotine izifiso kunye neempawu zokurhoxisa, ukuxhasa abantu kwimigudu yabo yokuyeka ukutshaya.
Kutheni i-Rimonabant ibangela ukudakumba?
Iindlela ezichanekileyo apho i-Rimonabant inokukhokelela ekudakaleni ayiqondwa ngokupheleleyo.Nangona kunjalo, izifundo kunye neengxelo zeklinikhi ziye zacebisa unxibelelwano olunokwenzeka phakathi kokusetyenziswa kweRimonabant kunye nomngcipheko okhulayo wokudakumba kunye nezinye iziphumo zengqondo.
I-Rimonabant, njengomdlali ochasene ne-cannabinoid receptor antagonist, ivimbela umsebenzi we-CB1 receptors kwinkqubo ye-endocannabinoid. inkqubo ye-endocannabinoid, enokuba negalelo kutshintsho lweemvakalelo kunye nempilo yengqondo.
Ukongezelela, inkqubo ye-endocannabinoid ibandakanyeka kulawulo lweempendulo zoxinzelelo kunye nokuguqulwa kwee-neurotransmitters ezifana ne-serotonin, eyaziwayo ukuba idlala indima ebalulekileyo ekulawuleni isimo sengqondo.
Kubalulekile ukuba uqaphele ukuba iimpendulo zomntu ngamnye kumayeza zinokuhluka, kwaye akuyena wonke umntu othatha i-Rimonabant uya kuba nokudandatheka okanye iziphumo ezichaphazelekayo.Nangona kunjalo, ukwenzeka kokudakumba kunye nezinye iimpawu zengqondo ezinxulumene nokusetyenziswa kweRimonabant zikhokelela ekuhoxisweni kweziyobisi imarike kumazwe amaninzi.Ngoko ngoku mhlawumbi akukho lula ukuthenga i-Rimonabant Powder kwikhemesti yendawo.Ukuba ufuna ukuthenga i-Rimonabant Powder kwi-intanethi, nokuba baninzi abanikezeli bePowder yeRimonabant, kufuneka ukhethe ethembekileyo.
Ukuba unenkxalabo malunga nokudakumba okanye nayiphi na eminye imiba enxulumene nempilo yengqondo, kubalulekile ukubonisana nengcali yezempilo ukuze uvavanye kwaye ukhokele.
Ukuhoxiswa kweRimonabant kunye nophando oluqhubekayo
Ngenxa yenkxalabo yokhuseleko, ngakumbi imiphumo emibi yengqondo, i-Rimonabant ekugqibeleni yahoxiswa kwiimarike kumazwe amaninzi. Nangona kunjalo, uphando kunye nophuhliso lwamachiza olujoliswe kwinkqubo ye-endocannabinoid luyaqhubeka, lugxininise ekuphuhliseni ezinye iikhompawundi kunye nonyango olujongene nemida yeRimonabant. .
Uphando lwexesha elizayo lunokubandakanya ukucokisa ukuqonda kwenkqubo ye-endocannabinoid, ukuphonononga usetyenziso olunokwenzeka lwemodulation ye-endocannabinoid kwiimeko ezahlukeneyo zonyango, kunye nokuphuhlisa amayeza akhuselekileyo nasebenza ngakumbi kule ndawo.
Ungayithenga phi iRimonabant Powder?
Kubalulekile ukuba uqaphele nokuba zininzi i-Rimonabant Powder ezithengiswayo kwi-intanethi.Ayifumanekanga ngokulula ukuthenga okanye ukusetyenziswa komntu ngamnye.I-Rimonabant Powder isetyenziswa ngokukodwa kwizicwangciso zophando kunye nophuhliso, kubandakanywa neenkampani zamachiza kunye nelabhoratri, ngenjongo yokufunda ichiza. iipropati, ukuqhuba izilingo zangaphambili kunye nekliniki, kunye nokuqulunqa iimveliso ezintsha zamachiza.Ngenxa yokukhathazeka kokhuseleko kunye nemiphumo enokubakho, kubalulekile ukuthenga i-Rimonabant Powder ephezulu ukuze ugweme imiphumo emibi engadingekile.Indlela yokukhetha ukuveliswa kweRimonabant ethembekileyo, kufuneka uhlolisise i-HPLC yabo ezimeleyo kunye neengxelo ze-COA.I-AASRAW ngumthengisi othembekileyo wokuthembela. Sinikezela ngePowder yeRimonabant esemgangathweni. Ngeodolo yehoseyile yeRimonabant Powder, uya kufumana ixabiso elikhuphisanayo kakhulu.
Ingxelo yoVavanyo lwePowder yeRimonabant-HNMR
Yintoni i-HNMR kwaye Ikuxelela ntoni i-spectrum ye-HNMR?H I-Nuclear Magnetic Resonance (NMR) ispectroscopy bubuchule bokuhlalutya bekhemistri esetyenziswa kulawulo lomgangatho kunye nophando lokumisela umxholo kunye nokusulungeka kwesampulu kunye nobume bayo bemolekyuli. Umzekelo, i-NMR inokuhlalutya ngokobungakanani imixube equlathe iikhompawundi ezaziwayo. Kwiikhompawundi ezingaziwayo, i-NMR inokusetyenziselwa ukuthelekisa ngokuchasene neelayibrari ezibonwayo okanye ukuqikelela ulwakhiwo olusisiseko ngokuthe ngqo. Nje ukuba ulwakhiwo olusisiseko lwaziwe, i-NMR inokusetyenziselwa ukumisela ulungelelwaniso lwemolekyuli kwisisombululo kunye nokufunda iipropathi ezibonakalayo kwinqanaba lemolekyuli ezifana notshintshiselwano oluhambelanayo, utshintsho lwesigaba, ukunyibilika, kunye nokusasazwa.
Indlela yokuthenga i-Rimonabant Powder kwi-AASraw?
❶Ukuqhagamshelana nathi ngenkqubo yethu yokubuza nge-imeyile, okanye usishiyele inombolo yakho ka-whatsapp, ummeli wethu wenkonzo yabathengi (CSR) uya kuqhagamshelana nawe kwiiyure ezili-12.
❷Ukusinika ubungakanani obubuziweyo kunye nedilesi.
❸I-CSR yethu iya kukubonelela ngekoteyishini, ixesha lokuhlawula, inombolo yokulandelela, iindlela zokuthunyelwa kunye nomhla wokufika oqikelelweyo (ETA).
❹Intlawulo yenziwe kwaye iimpahla ziya kuthunyelwa kwiiyure ezili-12.
❺Impahla efunyenweyo kwaye unike izimvo.
Umbhali weli nqaku:
UGqr Monique UHong uthweswe isidanga kwiKholeji yase-UK Imperial yaseLondon kwiFakhalthi yezoNyango
Umbhali wephepha leJenali yeNzululwazi:
1. Shira Hirsch
ILabhoratri yokutyeba kunye neMetabolism, iPOB 12065, iYerusalem 9112001, kwaSirayeli
2. Dalal AlKhelb
Iziko lokuFumana iziyobisi, kwiYunivesithi yaseMntla-mpuma, eBoston, MA 02115, eU.SA
3. URobert Ettaro
ISebe le-Pharmacology kunye ne-Toxicology, i-Jacobs School of Medicine kunye ne-Biomedical Sciences, iYunivesithi yaseBuffalo, eBuffalo, NY, eU.SA.
4. Alessandra Porcu
ISebe leSayensi zeBiomedical, iYunivesithi yaseCagliari, 09042, Monserrato, Italy
Lo gqirha/ingcali yenzululwazi ayinakuvuma okanye ithethelele ukuthengwa, ukuthengiswa, okanye ukusetyenziswa kwale mveliso nangasiphi na isizathu. I-Aasraw ayinayo indibaniselwano okanye ubudlelwane, ichazwa okanye ngenye indlela, kunye nalo gqirha. Injongo yokucaphula lo gqirha kukuvuma, ukuvuma kunye nokuncoma uphando olupheleleyo kunye nomsebenzi wophuhliso owenziwe ngoososayensi abasebenza kule nto.
Ucaphulo
[1] Soyka M.”Rimonabant kunye nokudakumba.“Pharmacopsychiatry.2008 Sep;41(5):204-5.doi: 10.1055/s-2008-1078744.Epub 2008 Sep 1.PMID: 18763226
[2] Boyd ST, Fremming BA.” Rimonabant–umchasi okhethiweyo we-CB1.” Ann Pharmacother.2005 Apr;39(4):684-90.doi: 10.1345/aph.1E499.Epub 2005 Mar 8.PMID: 15755787
[3] uCurioni C, uAndré C.” IRimonabant yokutyeba kakhulu okanye ukutyeba kakhulu.
[4] Wierzbicki AS.” I-Rimonabant: i-endocannabinoid inhibition ye-syndrome ye-metabolic. 2006
[5] Cox SL.”I-Rimonabant hydrochloride: i-arhente yophando yolawulo lwemingcipheko ye-cardiovascular risk factor.”Drugs Today (Barc) .2005 Aug;41(8):499-508.doi: 10.1358/dot.2005.41.8.893709. PMID: 16234873
[6] Bifulco M,Grimaldi C,Gazzerro P,Pisanti S,Santoro A.”Rimonabant: ichiza nje lokuthomalalisa ukutyeba? Ubungqina bangoku kwiziphumo zayo ze-pleiotropic. "Mol Pharmacol.2007 Jun; 71(6): 1445-56.doi: 10.1124 / mol.106.033118.
