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1 kits (10 Vials)
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▎ PT 141 Tsarin
Source: PubChem |
Jeri: Ac-Nle-cyclo(DHFRWK)-OH Tsarin kwayoyin halitta: C 50H 68N 14O10 Nauyin Kwayoyin Halitta: 1025.2g/mol Lambar CAS: 189691-06-3 Saukewa: 9941379 Synonyms: Bremelanotide |
▎ PT 141 Bincike
Menene asalin bincike na PT 141?
PT 141 shine analog na peptide na roba da kuma agonist na masu karɓar melanocortin, musamman ciki har da MC3R da MC4R, waɗanda aka fi sani da su a cikin tsarin kulawa na tsakiya [1] .Binciken PT 141 ya kawo sabon bege don maganin tabarbarewar jima'i. Nazarin farko a kan sa ya nuna cewa gudanar da PT 141 ga berayen da waɗanda ba na ɗan adam ba ya haifar da haɓakar penile erections. Bayan gudanar da tsarin tsarin ga berayen, an nuna kunnawar neurons a cikin hypothalamus ta karuwa a cikin c-Fos immunoreactivity. Neurons a cikin yanki guda na tsarin juyayi na tsakiya zasu dauki kwayar cutar pseudorabies da aka yi wa allurar a cikin corpus cavernosum na azzakari na bera [1] .PT 141 yana da damar magance tabarbarewar jima'i. Nazarin ya nuna cewa bayan gudanar da PT 141 ga maza na yau da kullum da marasa lafiya tare da rashin aiki na erectile, an sami karuwa mai sauri da kuma dogara da kashi a cikin ayyukan erectile. Wadannan sakamakon sun nuna cewa PT 141 yana da babban tasiri a matsayin sabon magani don rashin aikin jima'i [1].
Menene hanyar da PT 141 ke aiki akan masu karɓar melanocortin?
Ƙayyadaddun tsarin da PT 141 (Bremelanotide) ke aiki akan masu karɓar melanocortin yana da wuyar gaske, kuma mai zuwa shine cikakken bayani game da tsarin sa:
Tsarin mai karɓar melanocortin ya ƙunshi peptides na melanocortin, masu karɓa na musamman, sunadaran haɗe-haɗe, da masu adawa da endogenous. Melanocortin peptides ƙananan ƙwayoyin peptide ne waɗanda aka yi nazari a ƙarƙashin yanayi daban-daban na physiological da pathological. A halin yanzu, akwai sanannun nau'ikan masu karɓar melanocortin guda biyar, waɗanda aka rarraba a cikin tsarin juyayi na tsakiya da wasu kyallen takarda. G sunadaran melanocortin masu karɓa suna watsa sigina ta hanyar adenylate cyclase da sauran hanyoyin sigina na ƙasa. Dangane da ligand, yanayin bayyanar mai karɓar melanocortin, lokacin zama mai karɓa, sunadarai masu alaƙa, nau'in tantanin halitta, da sauran sigogi, hanyoyin siginar suna da rikitarwa da kuma pleiotropic. Kodayake duk masu karɓar melanocortin guda biyar an haɗa su zuwa Gs, ana iya haɗa su lokaci-lokaci zuwa Gq ko Gi [2].
Haɗin PT 141 zuwa masu karɓar melanocortin:
PT 141 shine analog na peptide. A matsayin melanocortin agonist mai karɓa, yana iya ɗaure ga masu karɓar melanocortin na tsakiya. PT 141, azaman analog na peptide na roba na α-melanocyte-stimulating hormone, shine agonist na masu karɓar melanocortin ciki har da MC3R da MC4R, waɗanda aka fi bayyana a cikin tsarin juyayi na tsakiya [1] .
Tasiri kan berayen mata:
A cikin berayen mata, PT 141 yana zaɓen yana motsa halayen jima'i ba tare da shafar lordosis, rhythm, ko wasu halayen jima'i ba. PT 141 baya haifar da kunna tsarin motsa jiki kuma baya shafar fahimtar ladan jima'i. Wannan yana nuna cewa tsarin melanocortin na tsakiya yana da mahimmanci wajen daidaita sha'awar mace. Ba a taɓa ba da rahoton zaɓin zaɓin ilimin likitanci akan halayen jima'i na berayen mata ba, wanda kuma ya sa PT 141 mai yuwuwar maganin farko da aka gano wanda zai iya magance cututtukan sha'awar mata [3].
Tasiri a kan berayen da waɗanda ba na ɗan adam ba: Gudanar da PT 141 zuwa berayen da primates waɗanda ba na ɗan adam ba suna haifar da haɓakar penile erections. Gudanar da tsarin PT 141 yana kunna neurons a cikin hypothalamus na berayen, wanda aka bayyana azaman karuwa a cikin c-Fos immunoreactivity. Neurons a cikin yanki ɗaya na hypothalamus za su ɗauki kwayar cutar pseudorabies da aka yi wa allurar a cikin kogon corpus na azzakari na bera [3].
Illa ga mazajen mutum:
Gudanar da PT 141 zuwa maza na al'ada da marasa lafiya tare da rashin aiki na rashin ƙarfi yana haifar da haɓaka da sauri da dogaro da kashi a cikin ayyukan haɓaka. Sakamakon ya nuna cewa PT 141 ana sa ran ya zama sabon magani don lalata jima'i [3].
Tasiri kan Matan Dan Adam: A cikin matan da suka riga suka yi mazaje masu fama da matsalar sha'awar jima'i, bayan gudanar da maganin cikin hanci guda daya na Bremelanotide (watau PT 141), yawancin mata sun ba da rahoton matsakaici ko matsakaicin matakan sha'awar jima'i. Idan aka kwatanta da placebo, an sami ƙarin fitowa fili na ingantacciyar amsa game da jin daɗin al'aurar bayan jiyya na Bremelanotide. Daga cikin matan da suka yi ƙoƙarin yin jima'i a cikin sa'o'i 24 bayan jiyya, yawancin mata sun fi gamsu da matakin sha'awar jima'i bayan amfani da Bremelanotide idan aka kwatanta da placebo. Koyaya, bayan gwamnatin Bremelanotide, babu wani gagarumin canji a cikin vagin vaginal congestion lokacin kallon bidiyon batsa [4].
A ƙarshe, a matsayin melanocortin agonist mai karɓa, PT 141, ta hanyar ɗaure masu karɓa na melanocortin, yana haifar da nau'o'in ilimin lissafi daban-daban a cikin nau'in dabba da mutane, musamman ma suna taka muhimmiyar rawa wajen daidaita aikin jima'i.
Sakamakon-sakamakon amsawar PT-141 akan halayen jima'i a cikin ɗakunan bilevel. (Top) Tasiri kan roƙon mata da aka haɗa tare da estrogen da progesterone (EP) ko estrogen kaɗai (E kaɗai). Gwaje-gwaje na baya-bayan nan sun nuna cewa duka allurai na 100- da 200-g/kg sun haɓaka adadin roƙon sosai idan aka kwatanta da abubuwan sarrafa saline (ƙimar P) (Tsakiya) Tasirin taki a cikin mata waɗanda ke da EP ko E kaɗai. (A ƙasa) Tasiri akan ƙididdiga na lordosis a cikin mata waɗanda aka haɗa tare da EP ko E kaɗai. Bayanan suna nufin SEM. *, P | 0.05 daga sarrafawa.
Source:PubMed [3]
Menene takamaiman fa'idodin PT 141 ga ƙananan sha'awar jima'i da matsalolin mazakuta?
Inganta aikin erectile:
Yawancin karatu sun nuna cewa PT 141 yana da wani tasiri na warkewa a kan rashin aiki na maza. Misali, a wasu gwaje-gwaje na asibiti, an gano cewa yana iya haifar da erections penile [5] (Shadiack AM, 2007). A cikin binciken Phase IIb na masu ciwon sukari na maza da ke fama da rashin ƙarfi, an ba da marasa lafiya da bazuwar don karɓar placebo ko nau'i-nau'i daban-daban na PT 141. Sakamakon ya nuna cewa a cikin ƙungiyoyin da ke da mafi girma na PT 141 (12.5mg da 15mg), an sami ci gaba mai mahimmanci a cikin Ayyukan Erectile (EF) na yanki na Ƙungiyar Ƙasa ta Duniya (EF). [5] .
Hanyar da PT 141 ke inganta aikin mizani na iya zama alaƙa da matsayinsa na melanocortinergic melanocortinergic, ɗaure ga masu karɓar melanocortin a cikin tsarin juyayi na tsakiya, musamman a cikin hypothalamus. Wannan ɗaurin yana iya daidaita hanyoyin jijiyoyi masu alaƙa da haɓakawa, don haka haɓaka haɓakar azzakari [5] .
Kyakkyawan juriya da aminci:
Bisa ga kwarewar asibiti na Bremelanotide, gudanar da melanocortin agonists (irin su Bremelanotide) yana da kyau a jure shi [6] . Ba a haɗa shi da hypotension da aka lura tare da masu hana phosphodiesterase-5 na yanzu da aka yi amfani da su don maganin rashin barci.
Nazarin tasiri na asibiti:
Kimantawa a cikin batutuwan maza masu lafiya da marasa lafiya tare da tabarbarewar erectile:
Bayan gudanar da subcutaneous a cikin batutuwan maza masu lafiya da marasa lafiya tare da rashin ƙarfi (ED) waɗanda suka ba da rahoton ƙarancin amsa ga Viagra, an kimanta analog heptapeptide melanocortin PT 141 na cyclic [7] (Rosen RC, 2004). An yi amfani da allurai daga 0.3 zuwa 10 MG ga batutuwa maza masu lafiya, kuma allurai fiye da 1.0 MG sun haifar da amsa mai mahimmanci mai mahimmanci. Marasa lafiya na ED sun sami placebo, 4 ko 6mg PT 141 a cikin ƙirar giciye a gaban haɓakar jima'i na gani (VSS). A duka allurai biyu, amsawar da aka samu daga PT 141 ya haifar da mahimmancin ƙididdiga. PT 141 yana da aminci kuma an jure shi sosai a cikin duka karatun. A cikin marasa lafiya waɗanda ba su da cikakkiyar amsa ga masu hanawa na PDE5, yiwuwar haɓaka, haƙuri, da ikon PT 141 don haifar da haɓaka mai mahimmanci suna nuna cewa PT 141 na iya ba da wani zaɓi na magani ga ED don yiwuwar yawan marasa lafiya.
Sakamakon haɗuwa tare da sildenafil:
Marasa lafiya goma sha tara wadanda suka ba da rahoton amsa ga Viagra ko Levitra an ba su 25mg sildenafil da 7.5mg intranasal PT 141, 25mg sildenafil da intranasal placebo spray, da kuma allunan placebo da intranasal placebo spray a cikin wani bazuwar crossover zane [8 , 200 LE]. RigiScan ya kimanta martanin da ba a taɓa gani ba ga abubuwan motsa jiki na gani na mintuna 30 na gani. Sakamakon ya nuna cewa amsawar da aka samu ta hanyar haɗin PT 141 da sildenafil ya fi girma fiye da abin da sildenafil kawai ya haifar. Haɗin ya kasance lafiyayye kuma an jure shi sosai, ba tare da haifar da sababbin abubuwan da ba su da kyau ko haɓaka a cikin mitoci ko tsananin abubuwan da ba su dace ba. Ƙarshen ita ce haɗuwa da intranasal PT 141 da phosphodiesterase 5 inhibitors na iya ba da zaɓin magani ga marasa lafiya waɗanda ba su da tasiri ko rashin haƙuri a mafi girma na maganin monotherapy.
Yin amfani da PT 141 yana da mahimmanci a fannoni da yawa, musamman kawo sabon bege ga yawancin marasa lafiya a fannin lafiyar jima'i. Ga matan da suka riga sun kasance masu fama da matsalar rashin sha'awar jima'i (HSDD), PT 141 babban ci gaba ne. A baya can, irin waɗannan marasa lafiya sukan jure matsi na tunani da ƙarancin sha'awar jima'i ke haifarwa a rayuwarsu ta yau da kullun, wanda ya shafi yanayin tunanin su da kuma kusancin dangantaka da abokan zamansu. Bayyanar PT 141 ya canza wannan yanayin. Ta hanyar daidaita hanyoyin da ke cikin kwakwalwa da ke cikin amsawar jima'i, yana inganta haɓaka sha'awar jima'i na marasa lafiya. Bayanan bincike na asibiti sun nuna cewa bayan yin amfani da Bremelanotide, akwai bambance-bambance a fili a cikin matsakaicin canje-canje na Ma'anar Ayyukan Jima'i na Mata - Desire domain (FSFI-D) da maki na 13th na Ma'aunin Matsalolin Jima'i na Mata - Desire / Arousal / Orgasm (FSDS-DAO) daga tushe zuwa ƙarshen binciken (EOS).
Wannan a hankali yana nuna kyakkyawan tasirinsa wajen haɓaka sha'awar jima'i na marasa lafiya da rage damuwa mai alaƙa, haɓaka ingancin rayuwar matan da suka riga suka yi maza tare da HSDD da taimaka musu su dawo da kwarin gwiwa da jin daɗin rayuwa.
Bugu da ƙari, PT 141 kuma yana nuna tasiri mai kyau akan rashin aikin jima'i na maza. Dangane da inganta ƙananan sha'awar jima'i na maza, yawancin marasa lafiya sun ba da rahoton karuwa mai yawa bayan amfani da shi, suna iya sake samun sha'awar jima'i. Sannan dangane da matsalolin mazakuta, wasu majinyatan aikin mazan jiya an inganta su zuwa wani matsayi bayan amfani da su, wanda hakan ke kara habaka tasirin azzakari, yana ba su damar kammala dabi'ar jima'i cikin kwanciyar hankali a cikin jima'i da inganta kwarewarsu ta jima'i.
Wannan babu shakka yana sauke nauyin jiki da tunani ga rukunin mazan da suka dade suna fama da tabarbarewar jima'i, yana gyara raunin tunani da matsalolin aikin jima'i ke haifarwa, sannan yana taimakawa wajen kiyaye daidaito da kwanciyar hankali na dangantakar iyali.
Daga macroscopic hangen nesa na binciken likita, yin amfani da PT 141 yana ba da shaida mai mahimmanci don bincike mai zurfi na hanyoyin da suka shafi lafiyar jima'i na ɗan adam.
Tsarin bincike na tsarin aikin sa ya sa masu bincike su gudanar da bincike mai zurfi game da hanyoyin jijiyoyi a cikin kwakwalwa da suka danganci amsa jima'i, masu karɓar melanocortin, da dai sauransu, inganta ci gaban bincike na asali a fannin lafiyar jima'i, aza harsashi don haɓaka ƙarin hanyoyin magani da magunguna don lalata jima'i, ƙara wadatar da taswirar likita a kan matsalolin kiwon lafiya, da kuma magance matsalolin jima'i.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jarida na Kimiyya Pfaus JG fitaccen ilimi mai alaƙa da manyan manyan cibiyoyi, gami da Jami'ar Charles Prague, Cibiyar Kiwon Lafiyar Jama'a ta Czech, Universidad Veracruzana, Jami'ar Concordia a Kanada, Jami'ar Rockefeller, da Jami'ar British Columbia. Bincikensa ya ƙunshi nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan binciken da bincikensa ya mai da hankali sosai kan Kimiyyar dabi'a, Kimiyyar Neurosciences & Neurology, Psychology, Endocrinology & Metabolism, da Urology & Nephrology.
A cikin fannin Kimiyyar Halayyar Hali, Pfaus yana bincika hadaddun ɗabi'u da hanyoyin su na asali. Ayyukansa a cikin Neurosciences & Neurology yana zurfafa cikin tsari da aiki na tsarin mai juyayi, yana ba da gudummawa ga fahimtar cututtukan cututtuka da hanyoyin tunani. A cikin Psychology, bincikensa na iya bincika tsarin ɗabi'a da tsarin tunani, yana ba da haske game da halayen ɗan adam da lafiyar hankali. A cikin Endocrinology & Metabolism, yana bincika tsarin hormonal da tafiyar matakai na rayuwa, mai yuwuwar haɗa waɗannan ayyukan nazarin halittu zuwa hali. Ayyukansa a cikin Urology & Nephrology zai iya mayar da hankali kan tsarin ilimin lissafi da ilimin cututtuka na tsarin urinary da kodan, mai yiwuwa ya binciko yadda waɗannan tsarin ke hulɗa tare da wasu ayyuka da halaye na jiki.
A duk tsawon aikinsa, James G. Pfaus yana yiwuwa ya buga takardu da yawa kuma ya ba da gudummawa sosai ga al'ummar kimiyya, tare da daidaita rata tsakanin fannonin kimiyya daban-daban da haɓaka bincike na tsaka-tsaki. Ayyukansa ba wai kawai yana haɓaka fahimtar fahimtar waɗannan fasahohin ba amma har ma yana da tasiri mai amfani ga kiwon lafiya da ci gaba da maganin warkewa. An jera Pfaus JG a cikin ambaton ambaton [3].
