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1 ngwa (10 Vials)
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▎ PT 141 Ọdịdị
Isi mmalite: PubChem |
Usoro: Ac-Nle-cyclo(DHFRWK)-OH Ụdị mkpụrụ ndụ: C 50H 68N 14O10 Arọ molekụla: 1025.2g/mol Nọmba CAS: 189691-06-3 PubChem CID: 9941379 Nkọwa okwu: Bremelanotide |
▎ PT 141 Nnyocha
Kedu ihe ndabere nyocha nke PT 141?
PT 141 bụ analog peptide sịntetik na agonist nke ndị na-anabata melanocortin, nke gụnyere MC3R na MC4R, bụ ndị a na-egosipụtakarị na usoro nhụjuanya nke etiti [1] . Nnyocha mbụ na ya gosiri na inye PT 141 oke na primates na-abụghị mmadụ mere ka ọ bụrụ erection penile. Mgbe nchịkwa usoro na oke, arụ ọrụ nke neurons na hypothalamus gosipụtara site na mmụba nke c-Fos immunoreactivity. Neurons nọ n'otu mpaghara nke sistemu ụjọ nke etiti ga-ebufe nje pseudorabies nke etinyere n'ime corpus cavernosum nke amụ oke [1] .PT 141 nwere ikike ịgwọ ọrịa mmekọahụ. Nnyocha egosiwo na mgbe inyechara PT 141 na ndị ikom na ndị ọrịa nwere nkwarụ erectile, enwere mmụba ngwa ngwa na nke dabere na dose na ọrụ erectile. Nsonaazụ ndị a na-egosi na PT 141 nwere ikike dị ukwuu dị ka ọgwụgwọ ọhụrụ maka arụrụ ọrụ mmekọahụ [1].
Kedu usoro nke PT 141 si eme na ndị na-anabata melanocortin?
Usoro a kapịrị ọnụ nke PT 141 (Bremelanotide) na-eme na ndị na-anabata melanocortin dị mgbagwoju anya, nke a bụ nkọwa zuru ezu nke usoro ya:
Sistemụ nnabata melanocortin nwere peptides melanocortin, ndị nnabata pụrụ iche, protein ngwa ngwa, na ndị na-emegide endogenous. Melanocortin peptides bụ obere homonụ peptide nke amụrụ n'okpuru ọnọdụ physiological na pathological dị iche iche. Ka ọ dị ugbu a, e nwere ụdị ndị na-anabata melanocortin ise a ma ama, nke na-ekesa na sistemụ ụjọ etiti na ụfọdụ anụ ahụ dị n'akụkụ. Ndị na-anabata protein melanocortin jikọtara ọnụ na-ebufekarị mgbaama site na adenylate cyclase na ụzọ mgbama mgbada ndị ọzọ. Dabere na ligand, ngosipụta elu nke melanocortin receptor, oge nnabata, protein ndị metụtara, ụdị cell, na paramita ndị ọzọ, ụzọ mgbaàmà dị mgbagwoju anya na pleiotropic. Ọ bụ ezie na ndị na-anabata melanocortin ise niile jikọtara na Gs, ha nwekwara ike jikọta ya na Gq ma ọ bụ Gi [2]..
Ejikọta PT 141 na ndị na-anabata melanocortin:
PT 141 bụ analog nke peptide. Dị ka melanocortin agonist receptor agonist, ọ nwere ike jikọta na etiti melanocortin receptors. PT 141, dị ka analog peptide synthetic nke α-melanocyte-stimulating hormone, bụ agonist nke ndị na-anabata melanocortin gụnyere MC3R na MC4R, bụ ndị a na-egosipụtakarị na usoro nhụjuanya nke etiti [1]. .
Mmetụta na oke ụmụ nwanyị:
N'ime oke ụmụ nwanyị, PT 141 na-ahọrọ nke ọma na-akpali omume mkpakọrịta nwoke na nwanyị na-enweghị emetụta lordosis, rhythm, ma ọ bụ omume mmekọahụ ndị ọzọ. PT 141 anaghị eme ka usoro moto rụọ ọrụ ma ghara imetụta echiche nke ụgwọ ọrụ mmekọahụ. Nke a na-egosi na usoro melanocortin etiti dị mkpa n'ịchịkwa agụụ mmekọahụ nke nwanyị. Mmetụta ọgwụ ahọpụtara na agụụ mmekọahụ nke oke ụmụ nwanyị ka akọpụtabeghị mbụ, nke na-emekwa PT 141 nwere ike bụrụ ọgwụ izizi amapụtara nwere ike ịgwọ ọrịa agụụ mmekọahụ nke nwanyị [3].
Mmetụta na oke na primates na-abụghị mmadụ: nchịkwa nke PT 141 na oke na ndị na-abụghị ụmụ mmadụ na-eduga na penile erections. Nlekọta usoro nke PT 141 na-arụ ọrụ neurons na hypothalamus nke oke, gosipụtara dị ka mmụba na c-Fos immunoreactivity. Neurons n'otu mpaghara nke hypothalamus ga-eburu nje pseudorabies nke a gbabara n'ime cavernosum corpus nke amụ oke [3].
Mmetụta na ụmụ nwoke:
Nlekọta nke PT 141 nye ndị nwoke nkịtị na ndị ọrịa nwere arụ ọrụ erectile na-eduga na mmụba ngwa ngwa na nke dabere na dose na ọrụ erectile. Nsonaazụ na-egosi na PT 141 na-atụ anya ka ọ bụrụ ọgwụgwọ ọhụrụ maka arụrụ ọrụ mmekọahụ [3].
Mmetụta n'ahụ ụmụ nwanyị mmadụ: N'ime ụmụ nwanyị na-amụbabeghị anya nwere nsogbu agụụ mmekọahụ, mgbe nchịkwa intranasal nke Bremelanotide gasịrị (ya bụ, PT 141), ọtụtụ ụmụ nwanyị na-akọ oke oke ma ọ bụ oke agụụ mmekọahụ. E jiri ya tụnyere placebo, e nwere omume pụtara ìhè karịa nke nzaghachi dị mma gbasara mmetụta nke agụụ mmekọahụ mgbe ọgwụgwọ Bremelanotide gasịrị. N'ime ụmụ nwanyị ndị nwara inwe mmekọahụ n'ime awa 24 ka a gwọchara ha, ọtụtụ ụmụ nwanyị nwere afọ ojuju maka oke agụụ mmekọahụ mgbe ha jiri Bremelanotide tụnyere placebo. Otú ọ dị, mgbe nchịkwa nke Bremelanotide gasịrị, ọ dịghị mgbanwe dị ịrịba ama na vaginal vaginal congestion mgbe ị na-ekiri vidio ndị gba ọtọ [4].
N'ikpeazụ, dị ka melanocortin agonist receptor PT 141, site na ijikọta melanocortin receptors, na-emepụta mmetụta dị iche iche nke anụ ahụ na ụdị anụmanụ na ụmụ mmadụ, karịsịa na-arụ ọrụ dị mkpa n'ịhazi ọrụ mmekọahụ.
Mmetụta nzaghachi dose nke PT-141 na omume mmekọahụ na ụlọ bilevel. (N'elu) Mmetụta na ịrịọ arịrịọ na ụmụ nwanyị nwere estrogen na progesterone (EP) ma ọ bụ estrogen naanị (E naanị). Nnwale post hoc gosipụtara na ma usoro 100- na 200-g/kg mụbara ọnụ ọgụgụ arịrịọ nke ukwuu ma e jiri ya tụnyere njikwa saline emeso ya (ụkpụrụ P | 0.05). (N'etiti) Mmetụta na ije ije na ụmụ nwanyị nwere EP ma ọ bụ E naanị. (N'okpuru) Mmetụta dị na lordosis quotients na ụmụ nwanyị nwere EP ma ọ bụ E naanị. Data bụ pụtara SEM. *, P | 0.05 site na njikwa.
Isi mmalite: PubMed [3]
Kedu uru PT 141 nwere ike ime maka agụụ mmekọahụ dị ala na ihe isi ike erectile?
Mmelite ọrụ erectile:
Ọtụtụ nchọpụta egosila na PT 141 nwere mmetụta ọgwụgwọ ụfọdụ na arụrụ ọrụ erectile nwoke. Dịka ọmụmaatụ, na ụfọdụ nnwale ụlọ ọgwụ, achọpụtara na ọ nwere ike ịkpalite erection penile [5] (Shadiack AM, 2007). N'ime nyocha nke Phase IIb nke ndị ọrịa na-arịa ọrịa shuga nke nwoke na-arịa ọrịa erectile, a na-ekenye ndị ọrịa na-enweghị usoro ka ha nweta placebo ma ọ bụ doses dị iche iche nke PT 141. Nsonaazụ gosiri na n'ime ìgwè ndị nwere oke doses nke PT 141 (12.5mg na 15mg), enwere ọganihu dị ịrịba ama na erectile Function (EF) ngalaba nke International Function (EF) dị iche iche nke International Function (EF). [5] .
Usoro nke PT 141 na-eme ka ọrụ erectile dịkwuo mma nwere ike jikọta ya na ọrụ ya dị ka ọgwụ melanocortinergic, na-ejikọta ndị na-anabata melanocortin na usoro nhụjuanya nke etiti, karịsịa na hypothalamus. Njikọ a nwere ike ịhazi ụzọ akwara ndị metụtara nrụpụta, si otú a na-akwalite nrụpụta penile [5] .
Ezigbo nnabata na nchekwa:
Dị ka ahụmahụ ahụike nke Bremelanotide si kwuo, nchịkwa nke melanocortin agonists (dị ka Bremelanotide) na-anabata nke ọma [6] . Ejikọtaghị ya na hypotension hụrụ ya na ndị na-emechi phosphodiesterase-5 dị ugbu a na-eji maka ọgwụgwọ nke arụrụ arụ erectile.
Ọmụmụ mmetụta ụlọ ọgwụ:
Nlele n'ihe gbasara nwoke nwere ahụike yana ndị ọrịa nwere arụ ọrụ erectile:
Mgbe nchịkwa subcutaneous na ndị nwoke nwere ahụike na ndị ọrịa nwere nrụrụ erectile (ED) bụ ndị kọrọ nzaghachi ezughị ezu na Viagra, a na-enyocha cyclic heptapeptide melanocortin analog PT 141 [7] (Rosen RC, 2004). A na-enye ndị nwoke nwere ahụike usoro doses sitere na 0.3 ruo 10 mg, yana doses karịrị 1.0 mg rụpụtara nzaghachi erectile dị ịrịba ama. Ndị ọrịa ED natara placebo, 4 ma ọ bụ 6mg PT 141 n'ime ihe ngosi crossover na ọnụnọ nke mkpali mmekọahụ (VSS). Na usoro abụọ a, nzaghachi erectile nke PT 141 kpatara dị ịrịba ama. PT 141 dị mma na nke ọma na ọmụmụ ihe abụọ ahụ. N'ime ndị ọrịa na-enweghị nzaghachi zuru oke na ndị na-emechi PDE5, ikike erectile, nnabata, na ikike nke PT 141 na-eme ka ọkpụkpụ dị ịrịba ama na-atụ aro na PT 141 nwere ike ịnye nhọrọ ọgwụgwọ ọzọ maka ED maka ọtụtụ ndị ọrịa nwere ike.
Mmetụta nke ngwakọta na sildenafil:
Ndị ọrịa iri na itoolu na-arụ ọrụ erectile bụ ndị gosipụtara onwe ha nzaghachi na Viagra ma ọ bụ Levitra nyere 25mg sildenafil na 7.5mg intranasal PT 141, 25mg sildenafil na intranasal placebo spray, na placebo mbadamba na intranasal placebo spray na a randomized crossover design [8 , 2000] (Diamond LE). RigiScan tụlere nzaghachi erectile na mkpali agụụ mmekọahụ abụọ nkeji iri atọ. Nsonaazụ gosiri na nzaghachi erectile kpatara site na nchikota PT 141 na sildenafil dị nnọọ ukwuu karịa nke sildenafil kpatara naanị ya. Ngwakọta ahụ dị mma ma nabata nke ọma, na-emeghị ka ihe ọjọọ ọhụrụ ma ọ bụ mmụba na ugboro ole ma ọ bụ ogo nke omume ọjọọ. Nkwubi okwu bụ na nchikota nke intranasal PT 141 na phosphodiesterase 5 inhibitors nwere ike inye nhọrọ ọgwụgwọ maka ndị ọrịa na-adịghị arụ ọrụ ma ọ bụ nwee ndidi na-adịghị mma na nnukwu doses nke monotherapy.
Iji PT 141 mee ihe dị oke mkpa n'ọtụtụ akụkụ, karịsịa na-eweta olileanya ọhụrụ nye ọtụtụ ndị ọrịa na ngalaba ahụike mmekọahụ. Maka ụmụ nwanyị premenopausal na-ata ahụhụ site na nsogbu agụụ mmekọahụ enwetara na mkpokọta hypoactive (HSDD), PT 141 bụ nnukwu mpụta. Na mbụ, ndị ọrịa dị otú ahụ na-edikarị nrụgide uche nke uche nke agụụ mmekọahụ dị ala na ndụ ha kwa ụbọchị, nke na-emetụta ọnọdụ mmetụta uche ha na mmekọrịta chiri anya na ndị mmekọ ha. Mpụta nke PT 141 agbanweela ọnọdụ a. Site n'ịhazi ụzọ ndị dị na ụbụrụ na-etinye aka na nzaghachi mmekọahụ, ọ na-eme ka ọchịchọ mmekọahụ nke ndị ọrịa dịkwuo mma. Ihe nyocha nyocha nke ụlọ ọgwụ na-egosi na mgbe ejiri Bremelanotide mee ihe, e nwere ọdịiche doro anya na mgbanwe mgbanwe mgbanwe nke Ọrụ Mmekọ nwoke na nwanyị - Desire domain (FSFI-D) na akara 13th nke ihe nrịbama nke nsogbu mmekọ nwoke na nwanyị - Desire / Arousal / Orgasm (FSDS-DAO) site na ntọala ruo na njedebe nke ọmụmụ (EOS).
Nke a na-egosipụta nke ọma mmetụta ya n'ịkwalite agụụ mmekọahụ nke ndị ọrịa na ibelata nsogbu ndị metụtara ya, na-emeziwanye ndụ ụmụ nwanyị premenopausal nwere HSDD ma na-enyere ha aka inwetaghachi obi ike na ọ joyụ nke ndụ.
Ọzọkwa, PT 141 na-egosipụtakwa mmetụta dị mma na arụrụ ọrụ mmekọahụ nke nwoke. N'ihe banyere imeziwanye agụụ mmekọahụ dị ala nke nwoke, ọtụtụ ndị ọrịa kọrọ mmụba dị ukwuu mgbe ejiri ya mee ihe, na-enwe ike nwetaghachi mmasị ha na mmekọahụ. Na n'ihe banyere ihe isi ike erectile, ọrụ erectile ụfọdụ ndị ọrịa na-emeziwanye ruo n'ókè ụfọdụ ka ejiri ya mee ihe, na-eme ka mmetụta nke nrụpụta penile dịkwuo mma, na-enyere ha aka imecha omume mmekọahụ nke ọma na ndụ mmekọahụ na imeziwanye ahụmahụ mmekọahụ.
Ihe ịrụ ụka adịghị ya na nke a na-ewepụ ibu arọ anụ ahụ na nke uche maka ndị nwoke na-enwe nsogbu site na mmejọ mmekọahụ ruo ogologo oge, na-edozi nsogbu uche nke uche nke nsogbu ọrụ mmekọahụ kpatara, ma na-enyekwa aka ịnọgide na-enwe nkwekọ na nkwụsi ike nke mmekọrịta ezinụlọ.
Site na echiche macroscopic nke nyocha ahụike, iji PT 141 na-enye ihe akaebe bara uru maka nyocha miri emi nke usoro ndị metụtara ahụike nwoke na nwanyị.
Usoro nyocha nke usoro ihe omume ya kpaliri ndị nchọpụta ka ha mee nyocha miri emi nke ụzọ akwara ozi na ụbụrụ metụtara mmeghachi omume mmekọahụ, ndị na-anabata melanocortin, wdg, na-akwalite ọganihu nke nchọpụta bụ isi n'ọhịa nke ahụike mmekọahụ, na-atọ ntọala maka mmepe nke usoro ọgwụgwọ ndị ọzọ na ọgwụ ọjọọ maka mmekọahụ rụrụ arụ, na-eme ka ahụike akụ na ụba na-aga n'ihu maka nsogbu ahụike siri ike na ịṅụ ọgwụ ike.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị Pfaus JG bụ agụmakwụkwọ pụrụ iche jikọtara ya na ọtụtụ ụlọ ọrụ ama ama, gụnyere Mahadum Charles Prague, Czech National Institute of Mental Health, Universidad Veracruzana, Mahadum Concordia na Canada, Mahadum Rockefeller na Mahadum British Columbia. Nnyocha ya gbasara usoro mmụta dị iche iche, na-elekwasị anya na sayensị omume, Neurosciences & Neurology, Psychology, Endocrinology & Metabolism, na Urology & Nephrology.
N'ime mpaghara Sayensị omume, Pfaus na-enyocha omume dị mgbagwoju anya na usoro ha dị n'okpuru. Ọrụ ya na Neurosciences & Neurology na-abanye n'ime nhazi na ọrụ nke usoro ụjọ ahụ, na-enye aka na nghọta nke ọrịa nhụjuanya na usoro ọgụgụ isi. N'ime Psychology, nchọpụta ya nwere ike nyochaa usoro omume na usoro uche, na-enye nghọta banyere omume mmadụ na ahụike uche. Na Endocrinology & Metabolism, ọ na-enyocha usoro hormonal na usoro metabolic, nwere ike jikọta ọrụ ndị a na-ahụ maka ndụ na omume. Ọrụ ya na Urology & Nephrology nwere ike ilekwasị anya na akụkụ physiological na pathological nke usoro urinary na akụrụ, ikekwe na-enyocha otú usoro ndị a si emekọrịta na ọrụ na omume anụ ahụ ndị ọzọ.
N'ime oge ọrụ ya niile, James G. Pfaus nwere ike bipụtala ọtụtụ akwụkwọ ma nye aka n'ụzọ dị ukwuu na obodo ndị ọkà mmụta sayensị, na-eme ka ọdịiche dị n'etiti ngalaba sayensị dị iche iche na ịkwalite nchọpụta interdisciplinary. Ọrụ ya ọ bụghị nanị na-eme ka nghọta nke usoro ọmụmụ nke usoro ndị a dịkwuo mma kamakwa ọ na-enwe mmetụta bara uru maka nlekọta ahụike na mmepe nke ọgwụgwọ ọgwụgwọ. Edepụtara Pfaus JG na ntụaka ntụaka [3].
