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1kit (10Vial) .
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▎ PT 141 Struktrɔ
Sos: PubChem |
Sikεns: Ac-Nle-sayklo(DHFRWK)-OH Mɔlikul Fɔmula: C 50H 68N 14O10 Molikul Weyt: 1025.2g/mol CAS Nɔmba: 189691-06-3 PubChem CID: 9941379, ɛn di ɔda wan dɛn Di tin dɛn we gɛt di sem minin: Bremelanotide |
▎ PT 141 Risach
Wetin na di risach bakgrɔn fɔ PT 141?
PT 141 na sεntetik pεptida analכg εn agonist fכ melanocortin rεsεpכta dεm, mεntal wan inklud MC3R εn MC4R, we dεn de εksprεs bכku pan di sεntri nεv sεstem [1] .di diskכvri fכ PT 141 dεn bכn nyu op fכ di tritmεnt fכ sεkswal disfכnkshכn. di fכs stכdi dεm pan am sho se we dεn gi PT 141 to rat εn nכn-hכman praymat dεm i de mek di penis εrekshכn. afta sistεmik administreshכn to rat, di aktibכshכn fכ nyuron dεm na di haypothalamus bin dכn sho bay inkrεs pan c-Fos imyun riaktiviti. di nyuron dεm we de na di sem rijyכn na di sεntri nεv sεstem go tek di pseudorabies vayrus we dεn injεkt insay di kכpas kεvεnכs na di rat penis [1] .PT 141 gεt di pכtεnshal fכ trit sεkswal disfכnkshכn. stכdi dεn sho se afta dεn gi PT 141 to nכmal man dεm εn pasεnshכn dεm we gεt εrektil disfכnkshכn, i bin gεt rεpid εn dכz-dipεndεnt inkrεs pan εrektil aktiviti. dis rizulεt dεm sho se PT 141 gεt big pכtεnshal as nyu tritmεnt fכ sεkswal disfכnkshכn [1]..
wetin na di mεkanism we PT 141 de akt pan melanocortin risεptor dεm?
di spεsifi k mεkanism we PT 141 (Bremelanotide) de akt pan melanocortin rεsεpכta dεm na rεdi kכmpleks, εn di fכlכw na ditayl εlaborashכn fכ in mεkanism:
di melanocortin risεptor sistεm de kכnsis fכ melanocortin pεpti dεm, yunik rεsεpכta dεm, aksesori protin dεm, εn εndojεnik antagonist dεm. di mεlanכkכtin pεptida dεm na sכm sכm pεptida כmon dεm we dεn stכdi כnda difrεn fysiolojikal εn patכlayz kכndishכn dεm. naw, fayv tכp dεm de we dεn no fכ di melanocortin rεsεpכta dεm, we de sheb insay di sεntri nεv sεstem εn sכm pεrifεral tisu dεm. di g protin-kכpl melanokortin rεsεpכta dεm kin כlwayz transmit signal tru adenylate cyclase εn כda dכwnstrim signal path dεm. dipכnt pan di ligεnd, sכfayz εksprεshכn fכ di melanokortin rεsεpכta, rεsεpכta כkupeshכn tεm, asosiet protin dεm, sεl tכp, εn כda paramita dεm, di signal path dεm na kכmpleks εn pleiotropik. pan tap we כl di fayv melanocortin risεptor dεm de kכpl to Gs, wan wan tεm dεn kin kכpl bak to Gq כ Gi [2]..
di binding fכ PT 141 to melanocortin rεsεpכta dεm:
PT 141 na wan pεptida analכg. as melanocortin risεptor agonist, i kin biεn to sεntri melanocortin risεptor dεm. PT 141, as sεntetik pεptida analכg fכ α-melanosayt-stimulεt כmon, na agonist fכ melanocortin risεptor dεm we inklud MC3R εn MC4R, we dεn mεnli εksprεs insay di sεntri nεv sεstem [1]. .
Ifekt pan uman rat:
insay uman rat, PT 141 de sεlektivli stimulate kכt bihayvya we nכ de afekt lordosis, ritm, כ כda sεks bihayvya. PT 141 nכ de mek sistεmik mכtal aktibכshכn εn i nכ de afekt di prεsεpshכn fכ sεkswal riwכd. dis sho se di sεntri mεlanכkכtin sistεm imכtant fכ rεgεl di uman in sεks dεn want. di sεlektiv fכmakכlכjik ifekt pan di apetitiv sεkshכnal bihayv fכ uman rat dεm nכ bin nεva ripot bifo, we de mek bak PT 141 pכtεnshal fכ bi di fכs drog we dεn aydentify we ebul fכ trit uman sεkshכnal dεsכrd dεm [3]..
ifekt pan rat εn nכn-hכman praymat dεm: Administreshכn fכ PT 141 to rat εn nכn-hכman praymat dεm de mek di penis εrekshכn. sistεmik administreshכn fכ PT 141 de aktibכt nyuron dεm na di haypothalamus fכ rat, we de sho as inkrεs pan c-Fos imyun riaktiviti. di nyuron dεm we de na di sem rijyכn na di haypothalamus go tek di pseudorabies vayrus we dεn injεkt insay di kכpas kεvεrnosum fכ di rat penis [3]..
Di tin dɛn we kin apin to mɔtalman man dɛn:
we dεn gi PT 141 to nכmal man dεm εn pasεnshכn dεm we gεt εrektil disfכnkshכn de mek di εrektil aktiviti inkrεs kwik kwik wan εn dipεnd pan di dכz. di risal dεm sho se dεn de εkspεkt se PT 141 go bi nyu tritmεnt fכ sεkswal disfכnkshכn [3]..
Ifekt pan mכtalman uman dεm: Insay uman dεm we dεn gεt sεkswal arousal dizayd, afta dεn gi Bremelanotide intranasal singl dכz (dat na, PT 141), mכr uman dεm bin ripot mכdarεt כ hεy lεvεl dεm fכ sεks dεn want. We yu kɔmpia am wit di plesibo, i bin gɛt mɔ klia tren fɔ pɔsitiv rispɔns bɔt di filin dɛn we pɔsin kin gɛt we i de arousal afta Bremelanotide tritmɛnt. Na di uman dɛm we bin tray fɔ du mami ɛn dadi biznɛs insay 24 awa afta dɛn dɔn trit dɛn, signifyant mɔ uman dɛm bin satisfay mɔ wit di lɛvɛl we dɛn bin de du mami ɛn dadi biznɛs afta dɛn yuz Bremelanotide kɔmpia wit di plasɛbo. Bɔt afta dɛn gi Bremelanotide, nɔ bin chenj ɛni big chenj na di vagina vasocongestion we dɛn de wach rud rud pikchɔ ɔ fim dɛn [4]..
fכ kכnklud, as melanocortin rεsεpכta agonist, PT 141, bay we i de biεn to melanocortin risεptor dεm, de prodyuz difrεn fysiolojikal ifekt dεm na animal mכdel dεm εn mכtalman, spεshal wan we de ple imכtant rol fכ rεgεl sεks fכnshכn.
Doz–rεspכns ifekt dεm fכ PT-141 pan sεks bihayvya na bilevεl chεmba dεm. (Tכp) Efεkt pan sכlisiteshכn in uman dεm we dεn praym wit εstrojen εn prכjεstεron (EP) כ εstrojen nכmכ (E nכmכ). Post hoc tests rivεl se כl tu di 100- εn 200-g/kg dos dεm inkrεs di nכmba כf sכlisiteshכn sכmtεm kכmpεr to salin-trit kכntrכl (P valyu dεm <0.05). (Middle) Efεkt pan pacing in uman dεm we dεn prim wit EP כ E nכmכ. (Bottom) Efεkt pan lordosis quotients in uman dεm we dεn praym wit EP כ E nכmכ. Data na min SEM. *, P <0.05 frɔm kɔntrol.
Sos:PubMed [3] we dɛn pul am.
Wetin na di spεsifi k pכtεnshal bεnεfit dεm fכ PT 141 fכ man dεm lכw sεks dεnshכn εn erectile difikulti?
Improvement of di erectile fכnshכn:
plεnti stכdi dεn sho se PT 141 gεt sכm tεrapi ifekt pan man erectile dysfunction. fכ egzampl, insay sכm klinik trial dεm, dεn fכnshכn se i ebul fכ mek di penis εrekshכn [5] (Shadiack AM, 2007). Insay wan Faz IIb stכdi pan man dayabεtik pasεnshכn dεm wit εrektil disfכnkshכn, dεn bin randomly asaynd di pasεnshכn dεm fכ rεsכp plasεbo כ difrεn doz כf PT 141. Di risכlt sho se insay di grup dεm we gεt hכy doz כf PT 141 (12.5mg εn 15mg), wan sכm improvεmεnt bin de na di Erectile Fכnshכn (EF) domεn כf di Intεrnashכnal כf Erectile Fכnshכn (IIEF), wit klia difrɛns we yu kɔmpia am wit di plesibo grup [5]. .
di mεkanism we PT 141 de impruv di εrektil fכnshכn kin riliyt to in rol as melanocortinergic dכg, we de biεn to melanocortin rεsεpכta dεm na di sεntri nεv sεstem, spεshal wan na di haypothalamus. dis binding kin rεgεl di nyural path dεm we riliyt to εrekshכn, so dat de mek di penis εrekshכn [5] . .
Gud tolɛrabiliti ɛn sef:
akɔdin to di klinik ɛkspiriɛns fɔ Bremelanotide, di administreshɔn fɔ melanocortin agonists (lɛk Bremelanotide) kin telɛret fayn fayn wan [6] . i nכ de aכsכsiayt wit di haypotεnshכn we dεn obsεv wit di kכrant fכsfכdiεstεrayz-5 inhibito dεm we dεn de yuz fכ trit di εrektil disfכnkshכn.
Klinik ɛfɛkt stɔdi dɛn:
Evalueshɔn pan hεlty man pipul dεm εn pasεn dεm wit εrektil disfכnkshכn:
Afta sabkutan administreshכn in hεlty man sכbjεkt dεm εn pasεnshכn wit εrektil disfכnkshכn (ED) we ripot insufisεnt rεspכns to Viagra, di saykli hεptapεptida melanocortin analכg PT 141 bin evaluate [7] (Rosen RC, 2004). Dכz we de frכm 0.3 to 10 mg bin administret to hεlty man sכbjεkt dεm, εn dכz we pas 1.0 mg prodyuz wan stεdi sכm εrektil rεspכns. ED pasɛnt dɛn bin gɛt plasɛbo, 4 ɔ 6mg PT 141 insay wan krɔs ɔva dizayn insay di prɛzɛns fɔ vijual sɛkshɔnal stimulashɔn (VSS). At di tu doz, di erectile rispכns we PT 141 indyuz bin stεdi sכmtin. PT 141 bin sef ɛn dɛn bin tolɛret am fayn fayn wan insay ɔl tu di stɔdi dɛn. Insay pasɛnt dɛn we nɔ bin gɛt adekwayt rispɔns to PDE5 inhibito dɛn, di ɛriktil pɔtɛnɛshɛl, tolɛrabiliti, ɛn abiliti fɔ PT 141 fɔ mek signifyant ɛrekshɔn sho se PT 141 kin gi ɔda tritmɛnt opshɔn fɔ ED fɔ wan pɔtɛnɛshɛl wayd rɛnj ɔf pasɛnt dɛn.
Efεkt כf kכmbaynshכn wit sildenafil:
Nayntin erectile dysfunction pasɛnt dɛn we dɛnsɛf ripɔt wan rispɔns to Viagra ɔ Levitra, dɛn gi dɛn 25mg sildenafil ɛn 7.5mg intranasal PT 141, 25mg sildenafil ɛn intranasal plasɛbo sprɛy, ɛn plasɛbo tablɛt ɛn intranasal plasɛbo sprɛy insay wan randomiz kros-ɔva dizayn [8] (Diamond LE, 2005). Di erectile rispכns to tu 30 minit vijual seksual stimulashכn dεm bin evaluate bay RigiScan. di risalts sho se di erectile rispכns we di kכmbaynshכn fכ PT 141 εn sildenafil indyuz bin sכmtεm pas di wan we sildenafil nכmכ indyuz. Di kɔmbayn bin sef ɛn dɛn bin de tolɛret am fayn fayn wan, we nɔ bin mek nyu bad bad tin dɛn apin ɔ inkris pan di frɛkuɛns ɔ di kayn bad bad tin dɛn we kin apin. di kכnklushכn na dat di kכmbaynshכn כf intranasal PT 141 εn phosphodiesterase 5 inhibitors kin gi tritmεnt opshכn fכ pasεnshכn dεm we nכ de wok כ we nכ gεt pwεl tכlerεns pan hכy dos כf mכnothεrapi.
Di yus fɔ PT 141 rili impɔtant pan bɔku tin dɛn, mɔ i de briŋ nyu op to bɔku pasɛnt dɛn we de du mami ɛn dadi biznɛs. Fɔ uman dɛn we dɔn pas 40 ia we de sɔfa wit akwyayz ɛn jenɛralized hypoactive sexual desire disorder (HSDD), PT 141 na big big tin we dɛn dɔn du. Bifo dis tɛm, bɔku tɛm dɛn kayn sik pipul ya bin de bia di prɛshɔn we dɛn kin gɛt bikɔs dɛn nɔ kin want fɔ du mami ɛn dadi biznɛs ɛvride, ɛn dis kin rili afɛkt di we aw dɛn de fil ɛn di tayt padi biznɛs we dɛn gɛt wit dɛn patna dɛn. Di we aw PT 141 kɔmɔt dɔn chenj dis sityueshɔn. bay we i de rεgεl di rod dεm na di bren we de involv fכ di sεks rεspכns, i de bכku bכku wan bכku di sikman dεm want fכ du mami εn dadi biznεs. Klinik risach data sho se afta yu yuz Bremelanotide, klia difrɛns de pan di avɛrej chenj dɛn na di Fem Sexual Function Index - Desire domain (FSFI-D) ɛn di 13th aytem skɔ na di Female Sexual Distress Scale - Desire/Arousal/Orgasm (FSDS-DAO) frɔm di beslayn to di ɛnd ɔf di stɔdi (EOS).
Dis intuitivli de sho in fayn fayn ifɛkt dɛm fɔ ɛp di pasɛnt dɛn fɔ want fɔ du mami ɛn dadi biznɛs ɛn fɔ stɔp di prɔblɛm we gɛt fɔ du wit am, fɔ rili impɔtant di kwaliti fɔ layf fɔ uman dɛn we nɔ gɛt HSDD bifo dɛn menopausal ɛn ɛp dɛn fɔ gɛt kɔnfidɛns bak ɛn di gladi at na layf.
pan tap dat, PT 141 de sho bak pכtεnshal pכsitiv ifekt dεm pan man sεks disfכnkshכn. We i kam pan fɔ mek man dɛn nɔ want fɔ du mami ɛn dadi biznɛs, bɔku pasɛnt dɛn bin ripɔt se dɛn dɔn bɔku afta dɛn dɔn yuz am, ɛn dɛn ebul fɔ gɛt intres bak fɔ du mami ɛn dadi biznɛs. Ɛn we i kam pan di prɔblɛm dɛn we kin mek dɛn ebul fɔ tinap tranga wan, dɛn dɔn mek sɔm pasɛnt dɛn ebul fɔ tinap fayn to sɔm mak afta dɛn dɔn yuz dɛn, we dɔn mek di ifɛkt we dɛn penis gɛt mɔ ɛn mɔ, we de mek dɛn ebul fɔ kɔmplit mami ɛn dadi biznɛs fayn fayn wan we dɛn de du mami ɛn dadi biznɛs ɛn we de mek dɛn ebul fɔ du mami ɛn dadi biznɛs fayn fayn wan.
Wi nɔ gɛt wan dawt fɔ se dis kin pul di bɔdi ɛn maynd lod fɔ di man grup we dɔn gɛt prɔblɛm wit mami ɛn dadi biznɛs fɔ lɔng tɛm, i kin mek di saykilɔjik trauma we kin kam bikɔs ɔf di prɔblɛm dɛn we gɛt fɔ du wit mami ɛn dadi biznɛs, ɛn i kin ɛp bak fɔ mek di famili gɛt wanwɔd ɛn stebul.
Frɔm makroskɔpik pɔynt fɔ mɛdikal risach, di yus fɔ PT 141 de gi valyu prɛktikal pruf fɔ dip ɛksplɔrɔshɔn fɔ di mɛkanism dɛn we gɛt fɔ du wit mɔtalman sɛkshɔnal wɛlbɔdi.
Di risach prɔses fɔ in mɛkanism fɔ akshɔn dɔn mek di risach pipul dɛn du mɔ dip ɛksplɔrɔshɔn fɔ di nyural path dɛm na di bren we gɛt fɔ du wit di sɛkshɔnal rispɔns, melanocortin riseptɔ, ɛn ɔda tin dɛm, fɔ protɛkt di prɔgrɛs we di bɛsik risach de du pan di fild fɔ sɛkshɔnal wɛlbɔdi, lay di fawndeshɔn fɔ divɛlɔp mɔ tritmɛnt we ɛn drɔgs fɔ sɛkshɔnal disfɔkshɔn, fɔ mek di mɛdikal trɔsri mɔ ɛn mɔ, ɛn tek wan sɔlid step fɔ go bifo fɔ mɛrɛsin fɔ win di prɔblɛm dɛn we gɛt fɔ du wit mami ɛn dadi biznɛs.
Bɔt di pɔsin we rayt di buk
Di tin dɛn we wi dɔn tɔk bɔt, na ɔl di tin dɛn we Cocer Peptides dɔn du risach, ɛdit ɛn kɔmpilayt.
Scientific Journal Author Pfaus JG na wan bigman we gɛt fɔ du wit bɔku bɔku big big institiushɔn dɛn, lɛk Chals Yunivasiti Prag, Chɛk Nashɔnal Instityut fɔ Mental Ɛlth, Yunivasiti Vɛrakruzana, Kɔnkɔdia Yunivasiti na Kanada, Rɔkfala Yunivasiti, ɛn di Yunivasiti ɔf British Kɔlumbia. In risach de span wan brayt spɛktrum ɔf disiplin dɛm, fɔs fɔ pe atɛnshɔn pan Bihayvya Sayns, Nyurosayns & Nyurɔlɔji, Saykoloji, Ɛndokrinɔlɔji & Mɛtabolism, ɛn Yurɔlɔji & Nɛfrɔlɔji.
Insay di eria fɔ Bihayvya Sayns, Pfaus de ɛksplɔrɔ kɔmpleks bihayvya ɛn dɛn ɔndalayn mɛkanism dɛm. in wok na Nyurosayns & Nyurolכji de dεl insay di strכkchכ εn fכnshכn fכ di nεv sεstem, we de kכntribyut fכ כndastand di nyurolכjik dizכrd dεm εn di kכgnitiv prכsεs dεm. Insay Sayikɔlɔji, in risach kin ɛgzamin di we aw pipul dɛn de biev ɛn di we aw dɛn de tink, we go gi tin dɛn fɔ no bɔt aw mɔtalman de biev ɛn di we aw dɛn de tink. insay Endocrinology & Metabolism, i de invεstigat כmon sistεm dεm εn mεtabolik prכsεs dεm, we kin lεnk dεn bayolojikal fכnshכn dεm ya to bihayvya. in wok na Yuroloji & Nεfroloji kin fכkus pan di fysiolojikal εn patכlayz aspek dεm fכ di urinary sistεm εn kidni dεm, i kin bi fכ εksplכr aw dεn sistεm ya de intarakt wit כda bכdi fכnshכn dεm εn bihayvya.
Tru in wok, i go mɔs bi se Jems G. Pfaus dɔn pablish bɔku pepa dɛn ɛn i dɔn ɛp bɔku pan di sayɛns kɔmyuniti, we dɔn briŋ difrɛns bitwin difrɛn sayɛns fild dɛn ɛn fɔ mek pipul dɛn du risach we gɛt fɔ du wit difrɛn difrɛn wok dɛn. In wok nɔ jɔs de advays di tiori ɔndastandin fɔ dɛn disiplin ya bɔt i gɛt prɛktikal implikashɔn fɔ wɛlbɔdi biznɛs ɛn di divɛlɔpmɛnt fɔ di tritmɛnt intavɛnshɔn dɛn. Pfaus JG de list insay di rεfrεns fכ saytεshכn [3].
