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1 pahu (10 Vials)
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▎ PT 141 Hoʻolālā
Puna: PubChem |
Kaʻina: Ac-Nle-cyclo(DHFRWK)-OH Hui Molekala: C 50H 68N 14O10 Kaumaha Molekala: 1025.2g/mol Helu CAS: 189691-06-3 PubChem CID: 9941379 Synonyms: Bremelanotide |
▎ PT 141 Imi
He aha ke kumu noiʻi o PT 141?
PT 141 mea he synthetic peptide analogue a me ka agonist o melanocortin receptors, nui me MC3R a me MC4R, i ka predominantly hōʻike 'ia i loko o ke kikowaena nūnū nenoai [1] .ʻO ka loaʻaʻana o PT 141 ua lawe mai i ka manaolana hou no ka mālamaʻana i ka moe kolohe. ʻO nā haʻawina mua ma ia mea i hōʻike ʻia ʻo ka lawelawe ʻana i ka PT 141 i nā ʻiole a me nā primates ʻole kanaka i alakaʻi i ka penile erections. Ma hope o ka lawelawe ʻana i nā ʻiole, ua hōʻike ʻia ka hoʻoulu ʻana o nā neurons i ka hypothalamus e ka hoʻonui ʻana i ka immunoreactivity c-Fos. ʻO nā neurons ma ka ʻāpana like o ka ʻōnaehana nūnū waena e lawe i ka maʻi pseudorabies i hoʻokomo ʻia i loko o ka corpus cavernosum o ka penis ʻiole [1] . Hiki i ka PT 141 ke mālama i ka maʻi kolohe. Ua hōʻike nā haʻawina ma hope o ka lawelawe ʻana i ka PT 141 i nā kāne maʻamau a me nā poʻe maʻi me ka erectile dysfunction, ua piʻi ka wikiwiki a me ka nui o ka nui o ka hana erectile. Hōʻike kēia mau hopena he mana nui ka PT 141 ma ke ʻano he lāʻau lapaʻau hou no ka maʻi kolohe [1].
He aha ke ʻano hana a PT 141 e hana ai i nā mea loaʻa melanocortin?
ʻO ka mīkini kikoʻī e hana ai ʻo PT 141 (Bremelanotide) i nā melanocortin receptors he paʻakikī, a ʻo kēia ka wehewehe kikoʻī o kāna hana:
ʻO ka ʻōnaehana melanocortin receptor nā melanocortin peptides, nā mea loaʻa kūʻokoʻa, nā protein komo, a me nā antagonists endogenous. ʻO Melanocortin peptides nā hormones peptide liʻiliʻi i aʻo ʻia ma lalo o nā kūlana physiological a me nā pathological. I kēia manawa, ʻelima mau ʻano ʻike o ka melanocortin receptors, ka mea i hoʻohele ʻia i loko o ka ʻōnaehana nūnū waena a me kekahi mau ʻiʻo peripheral. Hoʻouna pinepine nā mea loaʻa melanocortin i hui pū ʻia me ka protein G i nā hōʻailona ma o ka adenylate cyclase a me nā ala hōʻailona ʻē aʻe. Ma muli o ka ligand, ka ʻike ʻana o ka melanocortin receptor, ka manawa noho o ka mea hoʻokipa, nā protein pili, ke ʻano cell, a me nā ʻāpana ʻē aʻe, paʻakikī a pleiotropic nā ala hōʻailona. ʻOiai ua hui pū ʻia nā mea loaʻa melanocortin ʻelima i Gs, hiki ke hoʻohui ʻia i kekahi manawa me Gq a i ʻole Gi [2].
ʻO ka hoʻopaʻa ʻana o PT 141 i nā melanocortin receptors:
ʻO PT 141 kahi analog peptide. Ma ke ʻano he melanocortin receptor agonist, hiki iā ia ke hoʻopaʻa i nā mea loaʻa melanocortin waena. ʻO PT 141, ma ke ʻano he peptide analog o α-melanocyte-stimulating hormone, he agonist o nā melanocortin receptors me MC3R a me MC4R, ka mea i hōʻike nui ʻia i loko o ka ʻōnaehana nūnū waena [1] .
Nā hopena i nā ʻiole wahine:
Ma nā ʻiole wahine, hoʻoulu koho ʻo PT 141 i ke ʻano hoʻokamakama me ka ʻole o ka pili ʻana i ka lordosis, rhythm, a me nā ʻano moe kolohe ʻē aʻe. ʻAʻole hana ʻo PT 141 i ka hoʻoulu ʻana o ka ʻōnaehana a ʻaʻole pili i ka ʻike o ka uku moe kolohe. Hōʻike kēia he mea nui ka ʻōnaehana melanocortin waena i ka hoʻoponopono ʻana i ka makemake wahine. ʻAʻole i hōʻike mua ʻia ka hopena pharmacological koho i ka moe kolohe o nā ʻiole wahine, ʻo ia hoʻi ka PT 141 ka mea i ʻike mua ʻia i ka lāʻau lapaʻau i hiki ke mālama i nā maʻi makemake moe wahine [3].
Nā hopena ma luna o nāʻiole a me nā primatesʻole kanaka: Ke alakaʻiʻana o PT 141 i nāʻiole a me nā primatesʻole e alakaʻi i nā penile. ʻO ka hoʻokele ʻōnaehana o PT 141 e hoʻāla i nā neurons i ka hypothalamus o nā ʻiole, i hōʻike ʻia e like me ka hoʻonui ʻana i ka immunoreactivity c-Fos. ʻO nā neurons ma ka ʻāpana like o ka hypothalamus e lawe i ka maʻi pseudorabies i hoʻokomo ʻia i loko o ka corpus cavernosum o ka penis ʻiole [3].
Nā hopena i nā kāne kāne:
ʻO ka lawelawe ʻana o PT 141 i nā kāne maʻamau a me nā mea maʻi me ka erectile dysfunction alakaʻi i ka hoʻonui wikiwiki a hilinaʻi i ka nui o ka hana erectile. Hōʻike nā hopena i manaʻo ʻia ʻo PT 141 e lilo i lāʻau lapaʻau hou no ka male ʻana i ka wahine [3].
Nā hopena ma luna o nā wāhine kanaka: I nā wāhine premenopausal me ka maʻi hoʻoulu wahine, ma hope o ka hoʻohana ʻana i ka intranasal intranasal hoʻokahi o Bremelanotide (ʻo ia hoʻi, PT 141), ʻoi aku ka nui o nā wahine i hōʻike i ke kiʻekiʻe a i ʻole kiʻekiʻe o ka makemake moe. I ka hoʻohālikelike ʻia me ka placebo, ua ʻike ʻia ke ʻano o nā pane maikaʻi e pili ana i nā manaʻo o ka hoʻāla ʻana ma hope o ka mālama ʻana iā Bremelanotide. Ma waena o nā wahine i hoʻāʻo i ka moekolohe i loko o 24 mau hola ma hope o ka mālama ʻana, ʻoi aku ka nui o nā wahine i hauʻoli i ke kiʻekiʻe o ka hoʻoulu ʻana ma hope o ka hoʻohana ʻana iā Bremelanotide i hoʻohālikelike ʻia me ka placebo. Eia naʻe, ma hope o ka lawelawe ʻana iā Bremelanotide, ʻaʻohe loli nui i ka vasocongestion vaginal i ka wā e nānā ana i nā wikiō ponokala [4].
I ka hopena, ma ke ʻano he melanocortin receptor agonist, PT 141, ma ka hoʻopaʻa ʻana i nā melanocortin receptors, hoʻopuka i nā hopena physiological like ʻole i nā ʻano holoholona a me nā kānaka, ʻoi aku ka hana nui i ka hoʻoponopono ʻana i ka hana moekolohe.
Nā hopena hopena-pane o PT-141 ma ka moekolohe ma nā keʻena bilevel. (Ma luna) Nā hopena i nā noi i nā wahine i hoʻomaka me ka estrogen a me ka progesterone (EP) a i ʻole ka estrogen wale nō (E wale nō). Ua hōʻike ʻia nā hoʻāʻo post hoc ua hoʻonui ʻia ka nui o nā noi i hoʻohālikelike ʻia i nā mana mālama paʻakai (P values <0.05). (Middle) Nā hopena i ka pacing i nā wahine i hoʻomaka me EP a i ʻole E wale nō. (Ma lalo) Nā hopena i nā lordosis quotients i nā wahine i hoʻomaka me EP a i ʻole E wale nō. ʻO ka ʻikepili ka SEM. *, P ＜0.05 mai ka mana.
Puna:PubMed [3]
He aha nā pono kūpono kūpono o PT 141 no nā kāne male haʻahaʻa makemake a me nā pilikia erectile?
Hoʻonui i ka hana erectile:
Ua hōʻike ʻia nā haʻawina he nui he hopena therapeutic ko PT 141 i ka male erectile dysfunction. No ka laʻana, i kekahi mau hoʻokolohua lapaʻau, ua ʻike ʻia e hiki ke hoʻoulu i ka penile erections [5] (Shadiack AM, 2007). Ma kahi haʻawina Phase IIb o nā maʻi maʻi diabetic kāne me ka erectile dysfunction, ua hoʻokaʻawale ʻia nā mea maʻi e loaʻa i kahi placebo a i ʻole nā mea like ʻole o PT 141. Ua hōʻike nā hopena i nā hui me nā kiʻekiʻe kiʻekiʻe o PT 141 (12.5mg a me 15mg), aia kahi hoʻomaikaʻi nui i ka Erectile Function (EF) domain o ka International Index of Erectile 5. .
ʻO ke ʻano hana e hoʻomaikaʻi ai ka PT 141 i ka hana erectile e pili ana i kāna hana ma ke ʻano he lāʻau melanocortinergic, e hoʻopaʻa ana i nā mea hoʻokipa melanocortin i loko o ka ʻōnaehana nerve waena, ʻoi loa i ka hypothalamus. Hiki i kēia hoʻopaʻa ʻana ke hoʻoponopono i nā ala neural e pili ana i ke kūkulu ʻana, pēlā e hoʻoikaika ai i ka penile kūkulu [5] .
ʻAi maikaʻi a palekana:
Wahi a ka ʻike lapaʻau o Bremelanotide, ua ʻae maikaʻi ʻia ka lawelawe ʻana o nā agonist melanocortin (e like me Bremelanotide ) . ʻAʻole pili ia me ka hypotension i ʻike ʻia me ka phosphodiesterase-5 inhibitors i hoʻohana ʻia no ka mālama ʻana i ka erectile dysfunction.
Nā haʻawina hopena lapaʻau:
Ka loiloi i nā kumuhana kāne olakino a me nā maʻi me ka erectile dysfunction:
Ma hope o ka hoʻokele subcutaneous i nā kāne kāne olakino a me nā maʻi me ka erectile dysfunction (ED) i hōʻike i ka pane ʻole i ka Viagra, ua loiloi ʻia ka cyclic heptapeptide melanocortin analog PT 141 [7] (Rosen RC, 2004). ʻO nā kumu mai ka 0.3 a hiki i ka 10 mg i lawelawe ʻia i nā kāne kāne olakino, a ʻoi aku ka nui o ka nui ma mua o 1.0 mg i kahi pane erectile koʻikoʻi. Ua loaʻa i nā poʻe maʻi ED kahi placebo, 4 a i ʻole 6mg PT 141 i kahi hoʻolālā crossover i mua o ka hoʻoulu ʻana i ka moe kolohe (VSS). Ma nā ʻāpana ʻelua, ʻo ka pane erectile i hoʻokomo ʻia e PT 141 he mea koʻikoʻi. Ua palekana a ʻae maikaʻi ʻia ʻo PT 141 i nā haʻawina ʻelua. I nā poʻe maʻi i loaʻa ʻole ka pane kūpono i ka PDE5 inhibitors, hiki i ka PT 141 ke hoʻokumu i nā hana nui e hiki ke hāʻawi i kahi koho lapaʻau ʻē aʻe no ED no kahi ākea ākea o nā maʻi.
Ka hopena o ka hui pū ʻana me ka sildenafil:
He ʻumikūmāiwa mau maʻi erectile dysfunction i hōʻike iā lākou iho i ka pane iā Viagra a i ʻole Levitra i hāʻawi ʻia i ka 25mg sildenafil a me 7.5mg intranasal PT 141, 25mg sildenafil a me ka intranasal placebo spray, a me nā papa placebo a me ka intranasal placebo spray i kahi hoʻolālā crossover randomized [8] (Diamond LE, 2005). Ua loiloi ʻia e RigiScan ka pane erectile i ʻelua mau minuke 30-minuke. Ua hōʻike nā hopena i ka pane erectile i hoʻokomoʻia e ka hui pūʻana o PT 141 a me ka sildenafil iʻoi aku ka nui ma mua o ka mea i hoʻokomoʻia e ka sildenafil wale nō. Ua palekana ka hui ʻana a ua ʻae maikaʻi ʻia, me ka ʻole o ka hoʻoulu ʻana i nā hanana pōʻino hou a i ʻole ka piʻi ʻana o ka pinepine a i ʻole ka paʻakikī o nā hanana ʻino. ʻO ka hopena, ʻo ka hui pū ʻana o intranasal PT 141 a me phosphodiesterase 5 inhibitors hiki ke hāʻawi i kahi koho lapaʻau no nā poʻe maʻi ʻaʻole maikaʻi ʻole a maikaʻi ʻole ka hoʻomanawanui ʻana i nā kiʻekiʻe o ka monotherapy.
He mea koʻikoʻi ka hoʻohana ʻana o PT 141 i nā ʻano he nui, ʻoi aku ka lawe ʻana i ka manaʻolana hou i nā poʻe maʻi he nui i ke ʻano o ke ola kino. No nā wahine premenopausal e loaʻa ana a me ka maʻi hypoactive sexual desire maʻi (HSDD), ʻo PT 141 kahi holomua nui. Ma mua, ua hoʻomanawanui pinepine kēlā mau maʻi i ke koʻikoʻi noʻonoʻo ma muli o ka makemake haʻahaʻa i ko lākou ola i kēlā me kēia lā, kahi i hoʻopilikia nui i ko lākou kūlana manaʻo a me nā pilina pili me kā lākou mau hoa. Ua hoʻololi ka puka ʻana o PT 141 i kēia kūlana. Ma ka hoʻoponopono ʻana i nā ala i loko o ka lolo e pili ana i ka pane ʻana i ka moekolohe, hoʻomaikaʻi nui ia i ka makemake moe o nā maʻi. Hōʻike ka ʻikepili noiʻi maʻi ma hope o ka hoʻohana ʻana iā Bremelanotide, aia nā ʻokoʻa ʻokoʻa o ka hoʻololi awelika o ka Female Sexual Function Index - Desire domain (FSFI-D) a me ka helu helu 13th o ka Female Sexual Distress Scale - Desire/Arousal/Orgasm (FSDS-DAO) mai ka papa kuhikuhi a hiki i ka hopena o ke aʻo ʻana (EOS).
Hōʻike kēia intuitively i kona hopena maikaʻi i ka hoʻonui ʻana i ka makemake moe kolohe o nā maʻi a me ka hoʻohaʻahaʻa ʻana i ka pilikia pili, hoʻomaikaʻi nui i ka maikaʻi o ke ola o nā wahine premenopausal me HSDD a kōkua iā lākou e loaʻa hou ka hilinaʻi a me ka hauʻoli o ke ola.
Eia kekahi, hōʻike pū ʻo PT 141 i nā hopena maikaʻi loa i ka hana ʻino kāne kāne. Ma keʻano o ka hoʻomaikaʻiʻana i ka makemake male kāne haʻahaʻa, ua hōʻike ka nui o nā maʻi i ka piʻi nui ma hope o ka hoʻohanaʻana, hiki iā lākou ke hoʻihoʻi i ko lākou hoihoi i ka hana moekolohe. A e pili ana i nā pilikia erectile, ua hoʻomaikaʻi ʻia ka hana erectile o kekahi mau mea maʻi ma hope o ka hoʻohana ʻana, e hoʻonui ana i ka hopena o ke kūkulu ʻana i ka penile, e hiki ai iā lākou ke hoʻopau i ka moe kolohe me ka maʻalahi i ke ola moe kolohe a me ka hoʻomaikaʻi ʻana i ko lākou ʻike moekolohe.
ʻO kēia ka mea e hoʻomaha ai i ke kaumaha o ke kino a me ka noʻonoʻo no ka hui kāne i hoʻopilikia ʻia e ka male ʻana i ka wahine no ka manawa lōʻihi, hoʻoponopono i ka trauma psychological i hoʻokumu ʻia e nā pilikia hana moe kolohe, a kōkua pū i ka mālama ʻana i ka lokahi a me ke kūpaʻa o ka pilina ʻohana.
Mai kahi hiʻohiʻona macroscopic o ka noiʻi olakino, hāʻawi ka hoʻohana ʻana o PT 141 i nā hōʻike kūpono kūpono no ka ʻimi hohonu ʻana i nā ʻano hana e pili ana i ke ola kino kanaka.
ʻO ke kaʻina noiʻi o kāna hana hana ua hoʻoikaika i ka poʻe noiʻi e hana i ka ʻimi hohonu ʻana o nā ala neural i ka lolo e pili ana i ka pane ʻana i ka moekolohe, melanocortin receptors, etc. pilikia.
No ka mea kakau
ʻO nā mea i ʻōlelo ʻia ma luna nei ua noiʻi ʻia, hoʻoponopono ʻia a hōʻuluʻulu ʻia e Cocer Peptides.
ʻO ka mea kākau moʻolelo ʻepekema ʻo Pfaus JG he kula kiʻekiʻe e pili ana i nā ʻoihana hanohano, me Charles University Prague, Czech National Institute of Mental Health, Universidad Veracruzana, Concordia University ma Kanada, Rockefeller University, a me ke Kulanui o British Columbia. ʻO kāna noiʻi ʻana i kahi ākea ākea o nā hoʻopaʻi, e kālele ana i ka Behavioral Science, Neurosciences & Neurology, Psychology, Endocrinology & Metabolism, a me Urology & Nephrology.
Ma ke aupuni o Behavioral Science, ʻimi ʻo Pfaus i nā ʻano paʻakikī a me kā lākou mau ʻano kumu. ʻO kāna hana ma Neurosciences & Neurology e komo i loko o ke ʻano a me ka hana o ka ʻōnaehana nerve, e hāʻawi ana i ka hoʻomaopopo ʻana i nā maʻi neurological a me nā kaʻina cognitive. I loko o Psychology, hiki i kāna noiʻi ke nānā i nā ʻano hana a me nā kaʻina noʻonoʻo, e hāʻawi ana i nā ʻike i ka ʻano kanaka a me ke olakino noʻonoʻo. Ma Endocrinology & Metabolism, ke noiʻi nei ʻo ia i nā ʻōnaehana hormonal a me nā kaʻina metabolic, hiki ke hoʻopili i kēia mau hana biological i ka ʻano. Hiki i kāna hana ma Urology & Nephrology ke nānā aku i nā ʻano physiological a me nā pathological o ka ʻōnaehana urinary a me nā puʻupaʻa, e ʻimi paha i ke ʻano o kēia mau ʻōnaehana me nā hana kino a me nā ʻano.
I loko o kāna ʻoihana, ua paʻi paha ʻo James G. Pfaus i nā pepa he nui a ua hāʻawi nui i ke kaiāulu ʻepekema, e hoʻopili ana i nā āpau ma waena o nā kula ʻepekema like ʻole a me ka hoʻoulu ʻana i ka noiʻi interdisciplinary. ʻAʻole wale kāna hana e holomua i ka ʻike kumu o kēia mau aʻo akā loaʻa pū kekahi i nā hopena kūpono no ka mālama olakino a me ka hoʻomohala ʻana i nā hana therapeutic. Ua helu ʻia ʻo Pfaus JG ma ka ʻōlelo kuhikuhi [3].
