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Pula ea Rimonabant

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mabitso a mangTlhaloso: SR141716, Acomplia, Zimulti

AASraw ke moetsi ea hloahloa oa Rimonabant Powder e hloekileng e nang le lab e ikemetseng le fektheri e kholo e le ts'ehetso, tlhahiso eohle e tla etsoa tlasa taolo ea CGMP le sistimi ea taolo ea boleng bo sebetsang. Tsamaiso ea phepelo e tsitsitse, litaelo tse peli tsa thekiso le tse rekisoang li amoheleha.Rea u amohela ho laela ho tloha ho AASraw!

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Video ea Rimonabant phofo

 


 

Raw Rimonabant phofo Litlhaku tsa motheo

Name: Rimonabant Powder (SR141716)
CAS: 168273-06-1
Molecular Formula: C22H21Cl3N4O
Boima ba 'mele: 463.8
Melt Point: 230 ° C - 240 ° C
Temp Temp Storage: Phofo -20°C 3 lilemo
Color: Phofo e bohlooho-tšoeu

 


Semelo sa Rimonabant

Histori ea histori ea Rimonabant e qalile ho elella bofelong ba 1990 le mathoasong a 2000 ha bafuputsi ba qala ho batlisisa tsamaiso ea endocannabinoid le liphello tsa eona tse ka 'nang tsa e-ba teng mekhoeng e sa tšoaneng ea' mele, ho kenyelletsa le taolo ea takatso ea lijo le ho leka-lekanya matla.

Nakong ena, bo-ramahlale ba ile ba tsebahatsa li-cannabinoid receptors 'meleng, tse tsejoang ka hore ke li-receptor tsa CB1, tse fumanehang haholo bokong le liseleng tsa peripheral. Li-receptor tsena li bapala karolo ea ho laola takatso ea lijo, ho ja lijo le ho sebelisa matla.

E susumetsoa ke kutloisiso e ntseng e eketseha ea ho kenya letsoho ha tsamaiso ea endocannabinoid taolong ea takatso ea lijo, lik'hamphani tsa meriana li ile tsa qala nts'etsopele ea bahanyetsi ba CB1 ba khethiloeng ho lebisa tlhokomelo ea botenya le maemo a amanang.

Ka 1999, k'hamphani ea Fora ea Sanofi-Synthélabo (eo hona joale e leng Sanofi) e ile ea qala ho hlahisa moriana o bitsoang Rimonabant. Rimonabant e ne e etselitsoe ho thibela li-receptor tsa CB1 ka mokhoa o ikhethileng, ho thibela ka katleho tšebetso ea sistimi ea endocannabinoid.

Liteko tsa meriana li ile tsa etsoa ho hlahloba katleho le polokeho ea Rimonabant tsamaisong ea botenya le mathata a amanang le metabolism. Lithuto li bonts'itse litholoana tse ts'episang, tse bonts'ang tahlehelo ea boima ba 'mele le ntlafatso ea maemo a kotsi a pelo, joalo ka maemo a cholesterol le ho hanyetsa insulin.

Ho itšetlehile ka liphello tse ntle tse tsoang litekong tsena, Rimonabant o ile a fumana tumello ea ho laola ka 2006 European Union tlas'a lebitso la khoebo Acomplia. E ne e le meriana ea pele e entsoeng ka ho khetheha bakeng sa phekolo ea botenya nakong ea lilemo tse fetang leshome.

Leha ho le joalo, ho sa tsotellehe katleho ea eona ea pele, Rimonabant e ile ea tobana le mathata le likhang. Litlaleho tsa litla-morao tsa kelello, tse kenyelletsang ho tepella maikutlong, ho tšoenyeha, le maikutlo a ho ipolaea, li hlahile nakong ea tlhahlobo ea morao-rao ea ho bapatsa. Ho tšoenyeha ka litlamorao tsena tse mpe ho lebisitse ho tlosoa ha Rimonabant 'marakeng linaheng tse' maloa, ho kenyeletsoa European Union ka 2008.

Ho tlosoa ha Rimonabant ho ile ha totobatsa bohlokoa ba ho hlahloba ka hloko polokeho le likotsi tse ka 'nang tsa e-ba teng tsa kelello tse amanang le lithethefatsi tse lebisang tsamaiso ea endocannabinoid. Le hoja Rimonabant e sa ka ea phethahatsa tšepiso ea eona ea pele e le meriana e khahlanong le botenya, e fane ka lintlha tsa bohlokoa mabapi le ho kopana ho rarahaneng pakeng tsa tsamaiso ea endocannabinoid le taolo ea metabolic.

Ho tloha ha Rimonabant e tlosoa, boiteko ba lipatlisiso bo 'nile ba tsoela pele ho hlahloba bokhoni ba phekolo ea ho lebisa tlhokomelo tsamaisong ea endocannabinoid, empa ka ho tsepamisa maikutlo ho hoholo ho hlahisa metsoako e fokotsang likotsi tsa kelello tse amanang le thibelo ea CB1 receptor.

Phofo ea Rimonabant

Rimonabant Powder ke ntho ea meriana e ileng ea fumana tlhokomelo bakeng sa tšebeliso ea eona e ka sebelisoang lefapheng la bongaka. Ke ea sehlopha sa lithethefatsi tse tsejoang ka hore ke li-cannabinoid receptor antagonists tse khethang. Qalong Rimonabant e ile ea ntlafatsoa e le meriana e khahlanong le botenya, e lebisang tsamaiso ea endocannabinoid ho thusa ho laola takatso ea lijo le boima ba 'mele.

Mofuta oa Powder oa Rimonabant o lumella ho sebetsana le ho hasana habonolo nakong ea mekhoa ea ho etsoa. Rimonabant Powder e qhibiliha hanyenyane ka metsing, ho bolelang hore e na le ho qhibiliha ho fokolang methapong ea metsi. Leha ho le joalo, e ka bonts'a ho qhibiliha ho betere ho li-solvents tse kang ethanol, methanol kapa propylene glycol. Litšobotsi tsa solubility tsa Rimonabant ke lintlha tsa bohlokoa nakong ea ntlafatso ea tlhahiso.

Mokhoa oa ts'ebetso oa Rimonabant

Mokhoa oa ts'ebetso oa Rimonabant o kenyelletsa ho sebelisana ha oona le tsamaiso ea endocannabinoid 'meleng. Rimonabant ke mohanyetsi ea khethiloeng oa cannabinoid receptor, haholo-holo e lebisang ho li-receptor tsa CB1 tse fumanoang bokong le liseleng tsa peripheral.

Ha e kenngoa, Rimonabant e tlama le ho thibela li-receptor tsa CB1, ho thibela ts'ebetso ea li-receptor tsena ka li-cannabinoids tse sa feleng tse kang anandamide. Ka ho thibela li-receptor tsa CB1, Rimonabant e fetola mosebetsi oa tsamaiso ea endocannabinoid, e phethang karolo ea mekhoa e sa tšoaneng ea 'mele, ho kenyelletsa le taolo ea takatso ea lijo, ho leka-lekanya matla le metabolism ea lipid.

Ka ho khetheha, thibelo ea li-receptor tsa CB1 ke Rimonabant e ama tse latelang:

Taolo ea Takatso ea takatso ea lijo

Li-receptor tsa CB1 li kenya letsoho taolong ea takatso ea lijo le ho ja lijo. Ha li-receptor tsa CB1 li kentsoe tšebetsong, li hlohlelletsa tokollo ea li-neuropeptides tse bakang tlala le ho eketsa thepa e putsang ea lijo. Thibelo ea Rimonabant ea li-receptor tsa CB1 e fokotsa ts'ebetso ea sistimi ea endocannabinoid, e lebisang ho fokotseng takatso ea lijo le ho fokotsa ho ja lijo.

Tšebeliso ea Matla

Sistimi ea endocannabinoid e susumetsa tšebeliso ea matla ka ho laola thermogenesis, mokhoa oo 'mele o hlahisang mocheso le ho chesa likhalori. Ka ho thibela li-receptor tsa CB1, Rimonabant e ka 'na ea khothalletsa ho eketseha ha tšebeliso ea matla, e leng se tlatsetsang ho lahleheloa ke boima ba' mele.

Metabolism ea lipid

CB1 receptor activation e amahanngoa le ho eketseha ha lipogenesis (ho boloka mafura) le ho fokotseha ha lipolysis (ho senyeha ha mafura). Khahlano ea Rimonabant ea li-receptor tsa CB1 e ka fella ka ho hatelloa ha lipogenesis le ho phahamisa lipolysis, ho ka lebisang ho fokotseha ha ho bokellana ha mafura 'meleng.

Ke habohlokoa ho hlokomela hore le hoja Rimonabant e sebetsa haholo-holo e le mohanyetsi oa CB1 receptor, e ka boela ea bontša liphello tse ling tse eketsehileng kapa litšebelisano le li-receptor tse ling kapa litsamaiso 'meleng. Mekhoa e nepahetseng le liphello tsa Rimonabant li ka 'na tsa fapana' me e ntse e le taba ea lipatlisiso tse tsoelang pele.

Mokhoa oa ts'ebetso oa Powder ea Rimonabant o tšoana le oa Rimonabant ka mefuta e meng ea eona. Powder ea Rimonabant e bua ka mofuta oa Powdered oa moriana oa Rimonabant, e leng mohanyetsi ea khethiloeng oa cannabinoid receptor.

Ha Rimonabant Powder e tsamaisoa, ebang ke ka molomo kapa ka ho etsoa ka mefuta e fapaneng ea litekanyetso, e senyeha le ho kenngoa 'meleng. Ha e se e kenelletse, e sebelisana le sistimi ea endocannabinoid ka ho lebisa li-receptor tsa CB1 tse fumanehang bokong le liseleng tsa peripheral.

Liphello tsa Rimonabant ke life?

Rimonabant, moriana o thibelang botenya, qalong o ile oa ntlafatsoa ho thusa batho ba nang le bothata ba ho laola boima ba 'mele. Molemo oa eona o ka sehloohong e ne e le bokhoni ba eona ba ho thibela takatso ea lijo le ho khothalletsa ho theola boima ba 'mele. Ka ho khetheha, Rimonabant e ne e reretsoe ho sebelisoa merero e latelang:

Takatso ea ho ba le takatso ea lijo

Rimonabant e ne e etselitsoe ho fokotsa takatso ea lijo le ho khothalletsa tahlehelo ea boima ba 'mele ka ho thibela li-receptor tsa CB1 bokong tse amehang ho laola takatso ea lijo. Ka ho thibela li-receptor tsena, Rimonabant e ne e ikemiselitse ho fokotsa maikutlo a tlala le litakatso, ho thusa batho ho laola lijo tsa bona.

Bohloko ba ho Shoeloa Weight

Ka lebaka la khatello ea takatso ea lijo, Rimonabant e ne e lebeletsoe ho lebisa ho lahleheloa ke boima ba 'mele ho batho ba nang le botenya kapa botenya. Liteko tsa meriana li bontšitse hore phekolo ea Rimonabant e ka fella ka ho fokotsa boima ba 'mele ha ho kopantsoe le lijo tse laoloang le ho ikoetlisa.

Lintlafatso tsa Metabolism

Rimonabant e bontšitse melemo e ka bang teng ho ntlafatseng mekhoa ea metabolic e amanang le botenya, joalo ka profil ea lipid, ho hanyetsa insulin, le matšoao a kotsi ea pelo. E ne e reretsoe ho khothalletsa liphetoho tse ntle linthong tsena tsa metabolism, tse atisang ho senyeha ho batho ba boima bo feteletseng.

Thuso ea ho Khaotsa ho Tsuba

Rimonabant e ile ea fuputsoa bakeng sa tšebeliso ea eona e ka bang teng e le thuso ea ho khaotsa ho tsuba. Ho ne ho nahanoa hore ka ho thibela li-receptor tsa CB1, Rimonabant e ka fokotsa litakatso tsa nicotine le matšoao a ho tlohela, ho tšehetsa batho ka bomong boitekong ba bona ba ho khaotsa ho tsuba.

Ke hobane'ng ha Rimonabant e baka khatello ea maikutlo?

Mekhoa e tobileng eo Rimonabant e ka lebisang ho tepella maikutlong ha e utloisisoe ka botlalo. Leha ho le joalo, liphuputso le litlaleho tsa kliniki li bontšitse hore ho na le kamano e ka bang teng pakeng tsa tšebeliso ea Rimonabant le kotsi e eketsehileng ea ho tepella maikutlong le litla-morao tse ling tsa kelello.

Rimonabant, e le mohanyetsi ea khethiloeng oa cannabinoid receptor, e thibela mosebetsi oa li-receptor tsa CB1 tsamaisong ea endocannabinoid. Li-receptor tsa CB1 li phetha karolo ea mekhoa e sa tšoaneng ea 'mele, ho kenyelletsa le taolo ea maikutlo le ts'ebetso ea maikutlo. Ka ho thibela li-receptor tsa CB1, Rimonabant e ka senya ts'ebetso e tloaelehileng ea tsamaiso ea endocannabinoid, e ka tlatsetsang liphetohong tsa maikutlo le bophelo bo botle ba kelello.

Ho feta moo, sistimi ea endocannabinoid e kenya letsoho taolong ea likarabo tsa khatello ea maikutlo le ho feto-fetoha ha li-neurotransmitters tse kang serotonin, e tsejoang ka ho bapala karolo ea bohlokoa taolong ea maikutlo. Ho sitisoa ha lits'ebetso tsena ka ho hanyetsa ha li-receptor tsa CB1 ho ka baka matšoao a sithabetsang.

Ke habohlokoa ho hlokomela hore likarabo tsa motho ka mong ho meriana li ka fapana, 'me hase bohle ba noang Rimonabant ba tla ba le khatello ea maikutlo kapa litla-morao tse amanang le tsona. Leha ho le joalo, ketsahalo ea ho tepella maikutlong le matšoao a mang a kelello a amanang le tšebeliso ea Rimonabant e lebisitse ho tlosoa ha lithethefatsi 'marakeng linaheng tse' maloa. Kahoo hona joale ho ka 'na ha se ke ha e-ba bonolo ho reka Powder ea Rimonabant pharmacy ea moo. Haeba u batla ho reka Powder ea Rimonabant Inthaneteng, le hoja ho na le bafani ba bangata ba Rimonabant Powder, u lokela ho khetha e ka tšeptjoang.

Haeba u na le matšoenyeho mabapi le ho tepella maikutlong kapa mathata afe kapa afe a amanang le bophelo bo botle ba kelello, ho bohlokoa ho buisana le setsebi sa bophelo bo botle bakeng sa tlhahlobo e nepahetseng le tataiso.

Ho tlosoa ha Rimonabant le lipatlisiso tse tsoelang pele

Ka lebaka la mathata a tšireletso, haholo-holo litla-morao tsa kelello, Rimonabant o ile a qetella a tlosoa 'marakeng linaheng tse' maloa. Leha ho le joalo, lipatlisiso le nts'etsopele ea meriana e lebisitseng tsamaiso ea endocannabinoid e ntse e tsoela pele, e tsepamisitse maikutlo ho hlahisa metsoako e meng le mekhoa ea phekolo e sebetsanang le mefokolo ea Rimonabant.

Patlisiso ea nako e tlang e kanna ea kenyelletsa ho ntlafatsa kutloisiso ea sistimi ea endocannabinoid, ho hlahloba lits'ebetso tse ka bang teng tsa ho feto-fetoha ha endocannabinoid maemong a fapaneng a bongaka, le ho hlahisa meriana e sireletsehileng le e sebetsang haholoanyane lefapheng lena.

U ka reka Powder ea Rimonabant hokae?

Ke habohlokoa ho hlokomela esita le ho na le tse ngata tsa Rimonabant Powder tse rekisoang Inthaneteng. Ha e fumanehe habonolo bakeng sa ho rekoa kapa ho sebelisoa. Rimonabant Powder e sebelisoa haholo-holo litlhophisong tsa lipatlisiso le nts'etsopele, ho kenyeletsoa lik'hamphani tsa meriana le lilaboratori, ka sepheo sa ho ithuta thepa ea lithethefatsi, ho etsa liteko tsa pele le tsa bongaka, le ho etsa lihlahisoa tse ncha tsa lithethefatsi. Ka lebaka la mathata a ts'ireletso le litla-morao tse ka 'nang tsa e-ba teng, ke habohlokoa ho reka boleng bo phahameng ba Rimonabant Powder ho qoba litla-morao tse sa hlokahaleng. Mokhoa oa ho khetha moetsi ea ka tšeptjoang oa Rimonabant, o lokela ho hlahloba litlaleho tsa bona tse ikemetseng tsa HPLC le COA.AASRAW ke mofani ea ka tšeptjoang oa ho tšepa. Re fana ka boleng bo botle ba Rimonabant Powder. Bakeng sa liodara tse ngata tsa Rimonabant Powder, o tla fumana theko ea tlholisano haholo.

Tlaleho ea Tlhahlobo ea Powder ea Rimonabant-HNMR

HNMR ke eng hona HNMR spectrum e u bolella eng? H Nuclear Magnetic Resonance (NMR) spectroscopy ke mokhoa oa ho hlahloba k'hemistri o sebelisoang ho laola boleng le lipatlisiso bakeng sa ho fumana likahare le bohloeki ba sampuli hammoho le sebopeho sa limolek'hule. Mohlala, NMR e ka sekaseka ka bongata metsoako e nang le metsoako e tsebahalang. Bakeng sa metsoako e sa tsejoeng, NMR e ka sebelisoa ho bapisa le lilaebrari tsa spectral kapa ho fana ka sebopeho sa motheo ka kotloloho. Hang ha sebopeho sa motheo se tsejoa, NMR e ka sebelisoa ho fumana hore na limolek'hule li lumellana joang le tharollo hammoho le ho ithuta thepa ea 'mele boemong ba limolek'hule joalo ka phapanyetsano ea conformational, liphetoho tsa mohato, solubility le diffusion.

Mokhoa oa ho reka Powder ea Rimonabant ho tloha AASraw?

❶Ho ikopanya le rona ka sistimi ea rona ea ho botsa ka lengolo-tsoibila, kapa ho re siela nomoro ea hau ea WhatsApp, moemeli oa rona oa litšebeletso tsa bareki(CSR) o tla ikopanya le uena ka mor'a lihora tse 12.

❷ Ho re fa palo le aterese eo u e botsitseng.

❸ CSR ea rona e tla u fa khotheishene, nako ea ho patala, nomoro ea morao-rao, litsela tsa ho fihla, le letsatsi la ho fihla (ETA).

❹Ho lefa 'me thepa e tla romelloa ka mor'a lihora tse 12.

❺Lintho tse amohetsoeng le ho fana ka maikutlo.

Mongoli oa sengoloa sena:
Ngaka Monique Hong o fumane lengolo UK Imperial College London Faculty of Medicine

Sengoli sa pampiri sa Scientific Journal:
1. Shira Hirsch
Laboratori ea Botenya le Metabolism, POB 12065, Jerusalema 9112001, Israel
2. Dalal AlKhelb
Setsi sa ho Fumana Lithethefatsi, Univesithi ea Leboea-bochabela, Boston, MA 02115, USA
3. Robert Ettaro
Lefapha la Pharmacology le Toxicology, Jacobs School of Medicine le Biomedical Sciences, Univesithi ea Buffalo, Buffalo, NY, USA
4. Alessandra Porcu
Lefapha la Biomedical Sciences, Univesithi ea Cagliari, 09042, Monserrato, Italy
Ha ho ka tsela leha e le efe ngaka/saense ena e buellang kapa ho buella ho rekoa, thekiso, kapa tšebeliso ea sehlahisoa sena ka lebaka lefe kapa lefe. Aasraw ha e na kamano kapa kamano, ho boleloa kapa ho seng joalo, le ngaka ena. Sepheo sa ho qotsa ngaka ena ke ho ananela, ho ananela le ho babatsa lipatlisiso tse felletseng le mosebetsi oa nts'etsopele o entsoeng ke bo-ramahlale ba sebetsanang le ntho ena.

References

[1] Soyka M.”Rimonabant and depression.”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– mohanyetsi ea khethileng oa CB1.” Ann Pharmacother.2005 Apr;39(4):684-90.doi: 10.1345/aph.1E499.Epub 2005 Mar 8.PMID: 15755787

[3] Curioni C,André C.”Rimonabant bakeng sa boima bo feteletseng kapa botenya.” Cochrane Database Syst Rev.2006 Oct 18;2006(4):CD006162.doi: 10.1002/14651858.CD006162.pub2PM17054276IDXNUMX

[4] Wierzbicki AS.”Rimonabant: endocannabinoid inhibition for the metabolic syndrome.”Int J Clin Pract.2006 Dec;60(12):1697-706.doi: 10.1111/j.1742-1241.2006.01210.x. 17109677

[5] Cox SL.”Rimonabant hydrochloride: moemeli oa lipatlisiso bakeng sa taolo ea mabaka a kotsi a pelo.” Lithethefatsi Kajeno (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: ke sethethefatsi se thibelang botenya feela? Bopaki ba hajoale mabapi le litlamorao tsa eona tsa pleiotropic."Mol Pharmacol.2007 Jun;71(6):1445-56.doi: 10.1124/mol.106.033118.Epub 2007 Feb 27.PMID: 17327463


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