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▎ Melanotan-2 Ọdịdị
Isi mmalite: PubChem |
Usoro: Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-NH₂ Ụdị mkpụrụ ndụ: C 50H 69N 15O9 Ibu ibu: 1024.2 g/mol Nọmba CAS: 121062-08-6 PubChem CID: 92432 Ụdị okwu: MT-II |
▎ Melanotan-2 Nnyocha
Gịnị bụ ndabere nyocha nke Melanota?
Melanota bụ ihe analọgụ sịntetik. Ọ bụ ihe analog synthetic nke α-melanocyte-stimulating hormone (α-MSH), nke a kwadebere site na usoro njikọ kemịkal [1] . α-MSH bụ homonụ na-apụta n'okike nke nwere ọrụ physiological dị iche iche n'ime ahụ mmadụ, gụnyere ịhazi ụcha akpụkpọ ahụ. Emebere Melanota iji ṅomie ụfọdụ mmetụta α-MSH mana ọ nwere ọrụ siri ike yana ebumnuche ngwa akọwapụtara. Emepụtara Melanota na mbụ ka ọ bụrụ ihe na-akwalite ụcha akpụkpọ anụ, ya bụ, ihe a na-akpọ tanning. Site na mmụba nke ndị mmadụ na-achọ tanning, ụfọdụ ndị mmadụ malitere ịchọ inweta mmetụta na-agba ọchịchịrị ngwa ngwa site na ịgbanye Melanota. Nnyocha e mere na nke a na-elekwasị anya na usoro ya na mmetụta ya na pigmentation akpụkpọ ahụ. Dịka ọmụmaatụ, ọmụmụ achọpụtala na Melanota nwere ike jikọta ya na ndị na-anabata ya na melanocytes iji kpalite mmepụta nke melanin, si otú ahụ na-agbaji akpụkpọ ahụ [2, 3]..
Gịnị bụ Melanota?
Melanota bụ analọg sịntetik nke metụtara α-melanocyte-stimulating hormone (α-MSH). Isi ọrụ ya bụ ịbawanye ụcha akpụkpọ anụ na ime ka akpụkpọ ahụ mmadụ gbaa ọchịchịrị. Melanota na-egosipụtakarị mmetụta ya site na iso ndị na-anabata melanocortin na-emekọrịta ihe. Kpọmkwem, dị ka onye na-abụghị nke melanocortin receptor agonist, ọ nwere ike kpalie mmepụta nke melanin na akpụkpọ, si otú a nweta akpụkpọ pigmentation, ya bụ, tanning mmetụta. Na mgbakwunye, ọ nwekwara ike ịmepụta nrụpụta penile na-akpaghị aka na mmetụta mkpali mmekọahụ.
Gịnị bụ kpọmkwem usoro nke Melanota na tanning?
Melanota na-ebute ịcha akpụkpọ anụ site na imekọrịta ihe na melanocortin 1 receptor na melanocytes. A kwenyere na Melanota na-eṅomi mmetụta nke melanocortin α-melanocyte-stimulating hormone (α-MSH) na MC1 receptor nke melanocytes, na-ebute mmụba na nkwupụta nke protin na-egosi agouti. Melanota na-akpali melanocytes imepụta na nzuzo melanin, si otú ahụ na-amụba pigmentation akpụkpọ [4] . Ọ nwere ike ịkwalite mmepụta eumelanin na akpụkpọ ahụ iji nweta pigmentation akpụkpọ ahụ. Nnyocha egosiwo na α-melanocyte-stimulating hormone (α-MSH) analogue cyclic -[Ac-Nle (4), Asp (5), D-Phe (7), Lys (10)] alpha-MSH- (4 - 10) amide (Melanota), melanocortin nwere ike ime ka anụ ahụ na-eme ka e nwee agonist nke anụ ahụ . .
Kedu usoro a kapịrị ọnụ nke Melanota n'ịkwalite nrụpụta penile na ịkwalite mkpali mmekọahụ?
Mmalite nke erection:
N'ime oke anesthetized, Melanota - onye na-anabata melanocortin na-abụghị nke akọwapụtara - gosipụtara ntinye erectile dabere na dose mgbe a na-enye ya site na intravenous injections (0.1-1 mg / kg) ma ọ bụ hypothalamic paraventricular nucleus infusion (0.1-1 μg). Mmetụta a kpalitere erection penile ma belata nkwụsị nke ihe omume mbụ erectile [6] .Mmetụta ya nwere ike ịgụnye ime ka ndị na-anabata melanocortin rụọ ọrụ n'ime usoro nhụjuanya nke etiti, si otú ahụ na-achịkwa ụzọ ndị na-ahụ maka akwara metụtara ụlọ. Mgbe a na-agbanye Melanota intrathecally (0.2 μg) na ọkwa L6 - S1, njupụta nke ihe nrụpụta dị elu. Nke a na-egosi na ụzọ akwara dị na ọkwa azụ azụ nwekwara ike itinye aka na ntinye nke Melanota [6]..
Nkwalite nrụpụta:
Mgbe ịgba ọgwụ mgbochi nke Melanota (1 mg / kg), nzaghachi erectile na-akpata site na mkpali akwara cavernous na-abawanye, si otú a na-ekere òkè na-akwalite mmepụta [6] . Mgbe nnukwu mwepụ nke eriri ọmịiko paravertebral lumbar, a na-ewepụ mmetụta na-akwalite Melanota. Nke a na-egosi na mmetụta na-akwalite Melanota na nrụpụta na-adabere na iguzosi ike n'ezi ihe nke eriri ọmịiko paravertebral lumbar. N'ụzọ dị iche, Melanota gbara n'ime corpus cavernosum (1 μg) egosighi ọrụ nkwalite ọ bụla. Ntugharị azụ azụ ma ọ bụ ntụgharị nke abụọ nke akwara pelvic ma ọ bụ akwara azụ nke amụ emebighị ọrụ nkwalite nke Melanota intravenous (1 mg / kg), na-egosikwa na mmetụta na-akwalite Melanota n'elu mgbidi bụ site n'okporo ụzọ akwara ọmịiko karịa akwara pelvic ma ọ bụ akwara azụ [6] nke penis..
Mmalite omume mkpali ụmụ nwanyị:
Nnyocha achọpụtala na Melanota nwekwara mmetụta na omume mmekọahụ nke nwanyị. N'ime oke ụmụ nwanyị, oke ovariectomized pretreated with estradiol benzoate (EB) na progesterone (P), intravenous injections of Melanota (1 na 3 mg / kg) mụbara ọnụ ọgụgụ nke jumps, rushes, na ntị wiggles, na-egosi na progesterone nwere ike imekọ ihe na Melanota iji mụbaa omume agụụ mmekọahụ nke nwanyị [7]..
Mmetụta MTII na tumorigenicity nke mkpụrụ ndụ melanoma.
Isi mmalite: PubMed [1]
Melanota bụ ihe nwere ọtụtụ ọrụ yana ntụzịaka nyocha. Ihe na-esonụ ga-ewebata nchọpụta ndị ọzọ metụtara Melanota.
Mmalite nke erection:
N'ime nnyocha ụfọdụ, a chọpụtara na Melanota nwekwara mmetụta na usoro ọmụmụ. Dịka ọmụmaatụ, Melanota nwere ike ime ka ọkpụkpụ penile na-adịghị mma. Ụfọdụ ndị ọrịa nwetara erection na-egbu mgbu mgbe ntụtụ subcutaneous nke Melanota, ma gosipụtakwa ihe mgbaàmà nke mkpali akwara ọmịiko, dị ka ọnụọgụ obi na-arịwanye elu, ọbara mgbali elu, nkwụsịtụ, na ịsụsọ dị ukwuu [8] . Tụkwasị na nke ahụ, na ọmụmụ banyere òké, ihe ndị melanocortin nwere ike ime ka ọkpụkpụ lordosis, bụ nke a na-akọwa dị ka ihe àmà nke mmụba nke agụụ mmekọahụ [8] , na-atụ aro na mmetụta Melanota na usoro ọmụmụ nwere ike jikọta ya na mkpali mmekọahụ na nhazi nke omume mmekọahụ.
Nkwalite mmepụta nke melanin:
Dị ka synthetic melanocortin analogue, Melanota nwere ike jikọta na melanocortin I receptor (MC1R) iji kwalite mmepụta nke melanin [9] .Ọ na-emekarị nke a site n'ịkwalite mmụba nke melanocytes na ịhazi ọrụ nke tyrosinase. Mmetụta a nke ịkwalite mmepụta melanin na-enye Melanota uru ngwa ngwa n'ọhịa nke akpụkpọ ahụ, dịka ọmụmaatụ, ọ nwere ike ịrụ ọrụ na ọgwụgwọ na mgbochi nke ụfọdụ ọrịa anụ ahụ.
Nnyocha n'akụkụ mgbochi tumor:
N'ime nnyocha e mere na mgbochi tumor, ọmụmụ ihe na-eji B16-F10 melanoma model chọpụtara na ọ bụ ezie na Melanota enweghị mmetụta na mmụba nke mkpụrụ ndụ melanoma, ọ nwere ike igbochi mbugharị, mbuso agha, na ikike ịmepụta mkpụrụ ndụ melanoma. Ngwa mpaghara nke Melanota nwekwara ike belata ọganihu etuto ahụ na ụmụ oke nwere melanoma siri ike. Usoro ya bụ ime ka mmụba nke phosphatase na tensin homolog (PTEN) site na melanocortin 1 receptor (MC1R), si otú ahụ na-egbochi ọganihu nke melanoma site n'iwetu cyclooxygenase II (COX-2) / prostaglandin E2 (PGE2) ụzọ akara [1].
Mmetụta ọgwụgwọ na autism:
Ụfọdụ ọmụmụ na-eji ihe nrịbama nke nne na-alụso ọrịa ọgụ (MIA) nke autism iji nyochaa ike ọgwụgwọ nke melanocortin receptor 4 agonist M Melanota maka àgwà dị ka autism na ụmụ oke nwoke [10] . Nlekọta nke Melanota nye ụmụ oke MIA maka ụbọchị asaa na-esochi mere ka ọ dịkwuo mma na njirimara omume ọha mmadụ. Enweghị mgbanwe dị ịrịba ama na ihe ngosi omume mmekọrịta mmadụ na ụmụ oke C57 nwere ọdịdị nkịtị mgbe ọgwụgwọ Melanota gasịrị. Tụkwasị na nke ahụ, na ụmụ oke C57 nkịtị, ọ dịghị mgbanwe dị na nchekasị-dị ka ma ọ bụ omume ugboro ugboro mgbe ọgwụgwọ Melanota gasịrị, ma enwere mbelata dị ukwuu na arọ ahụ mgbe ọgwụgwọ subacute gasịrị. Data ndị a na-egosi na Melanota bụ ọgwụ dị irè nke nwere ike imeziwanye adịghị ike omume dịka autism na ụdị autism nke ụmụ oke nwoke MIA toro eto.
Mweghachi nke enweghị ncheta:
Nnyocha e mere egosiwo na nri nwere oke abụba (HF) egosila na ọ na-eme ka ihe ize ndụ nke mmebi akwara na ọrịa neurodegenerative dịkwuo elu. Ọmụmụ ihe a nyochara mmekọrịta dị n'etiti nri, Melanota na-ezubere ndị na-anabata melanocortin, na omume nke zebrafish [11] . N'ụzọ dị ịtụnanya, ọbụlagodi nri HF dị mkpụmkpụ nke dịruo ihe dịka 1% nke ndụ zebrafish nwere mmetụta mmepe siri ike. E jiri ya tụnyere zebrafish nyere nri nchịkwa, zebrafish nyere nri HF gosipụtara ebe nchekwa adịghị mma, ọkwa nchegbu na-abawanye, na mbelata ọchịchọ nyocha mgbe naanị izu atọ gachara. Melanota tụgharịrị ihe ọjọọ ndị a sitere na nri HF kpatara. Anụmanụ na-eri nri HF ma mesoo ya na Melanota gosipụtara ebe nchekwa, nchekasị, na omume nyocha dịka nke ndị otu njikwa. Ọmụmụ ihe a na-enye ihe àmà na ọbụna nri HF dị mkpirikpi nwere ike inwe mmetụta na ebe nchekwa na ọnọdụ, na ọ bụ nchọpụta mbụ iji gosi na Melanota nwere ike gbanwee mgbanwe ndị a.
Ụkpụrụ omume ọha mmadụ:
N'ihe gbasara nchọpụta neuroscience, a chọpụtara na Melanotan-II nwere ike ịhazi àgwà mmekọrịta site n'ịkwalite ndị na-anabata melanocortin wee mee ka usoro oxytocin Central [12] rụọ ọrụ . Kpọmkwem, mgbe nchịkwa sistemu nke Melanota gasịrị, ntụtụ intravenous karịa nchịkwa intranasal nke Melanota nwere ike ime ka okwu Fos pụta ìhè na magnocellular neurons nke supraoptic nucleus (SON) na paraventricular nucleus (PVN) nke hypothalamus, na nzaghachi a nwere ike ibelata site na pretreatment na melanocortin19. Ihe ndekọ eletrọnịkị egosila na ịgba ọgwụ mgbochi nke Melanota nwere ike ime ka ọnụọgụ nke neurons oxytocin dị na SON mụbaa. Nke a na-egosi na Melanota nwere mmetụta nchịkwa na usoro oxytocin metụtara mmekọrịta mmadụ na ibe ya na usoro ụjọ ahụ, na usoro ya nwere ike ịbụ ịhazi ọrụ na nzuzo nke neuron oxytocin site n'ịgbalite ndị na-anabata ya kpọmkwem na ụzọ mgbaàmà.
Nnyocha banyere oke ibu na ahụike metabolic:
N'ihe banyere oke ibu na ahụ ike metabolic, ụfọdụ ọmụmụ jiri ụdị mkpụrụ ndụ ihe nketa nke pituitary adenylate cyclase-activating polypeptide (PACAP) - ụmụ oke na-enweghị ike wee chọpụta na melanocortin agonist agonist Melanota nwere ike napụta akụkụ ahụ na-adịghị mma thermogenic ikike nke ụmụ oke na-enweghị PACAP n'oge mgbanwe oyi. Nke a na-egosi na PACAP nwere ike rụọ ọrụ dị elu nke usoro melanocortin, na-achịkwa ọrụ akwara ọmịiko nke anụ ahụ adipose na-acha aja aja na ụmụ oke, si otú ahụ na-enwe mmetụta na oke ibu na ahụike metabolic [13]..
Usoro nke metabolism na okpomọkụ nke ahụ:
Melanota nwekwara mmetụta dị ukwuu na usoro endocrine. Dịka ọmụmaatụ, nchịkwa intraperitoneal nke Melanota na ụmụ oke nwere ike ime ka hypometabolism / hypothermia dị omimi na nke na-agafe agafe [14] . Nnyocha egosiwo na ụmụ oke na-enweghị mkpụrụ ndụ mast, a na-ewepụ hypothermia nke Melanota kpatara, na-atụ aro na a chọrọ ntinye nke mkpụrụ ndụ mast. Melanota na-akpata hypothermia na ụmụ oke site na ịgbalite mkpụrụ ndụ mast ma na-akpali ndị na-anabata histamine 1, na usoro ya na-agụnye mmekọrịta nke ọtụtụ ihe endocrine na ndị na-anabata ya.
N'ikpeazụ, dị ka ihe sịntetik nke dọtara mmasị dị ukwuu, Melanota na-egosipụta àgwà pụrụ iche n'ọtụtụ ubi. N'ihe gbasara akpụkpọ ahụ, site na ijikọta kpọmkwem ndị na-anabata ya na melanocytes, ọ nwere ike ịkwalite mmepụta nke melanin nke ọma, na-enye usoro tanning na-abụghị omenala maka ndị na-achọ ka ọkpụkpụ ọla dị mma. E jiri ya tụnyere tanning site na ikpughe ogologo oge na ụzarị ultraviolet, Melanota nwere ike izere mmebi nke ụzarị ultraviolet na akpụkpọ ahụ ma belata ihe ize ndụ nke ntachu anwụ, ịka nká anụ ahụ, na ọbụna kansa anụ ahụ.
Site n'echiche nke nhazi ọrụ mmekọahụ, Melanota nwere mmetụta dị mma n'ịkwalite nrụpụta penile na-atụghị anya ya na ịkwalite mkpali mmekọahụ. Nke a bụ ihe ngwọta dị irè maka ụfọdụ ndị nwere nsogbu mmekọahụ ma ọ bụ ndị nwere olileanya imeziwanye ahụmahụ mmekọahụ ha. Ọ nwere ike nweta mmetụta dị mma na ọrụ mmekọahụ site n'ịkwalite ụzọ akwara ozi dị iche iche na usoro nhụjuanya nke etiti na nke dị n'akụkụ na ịhazi ndị na-ahụ maka ndị na-ahụ maka ndị na-ahụ maka ndị na-ahụ maka ihe na ndị na-anabata ya, na-enye ohere ọhụrụ maka ịkwalite ahụike mmekọahụ.
Na nyocha banyere oke ibu na ahụike metabolic, Melanota na-egosikwa uru ndị nwere ike. Ọ nwere ike na-achịkwa ike metabolism na ahụ okpomọkụ na nwere ụfọdụ mma mmetụta na adịghị arụ ọrụ nke adipose anụ ahụ na oke ibu. Ọ na-enye ntụziaka nyocha ọhụrụ maka ọgwụgwọ oke ibu na njikwa ahụike nke metabolic, nke na-enyere aka ịmepụta usoro ọgwụgwọ ọhụrụ na mmelite nke ọnọdụ ahụike nke ndị ọrịa buru ibu.
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
Cousen, P bụ onye na-eme nchọpụta na-elekwasị anya na ngalaba nke Allergy Dermatology. Ejikọtala ọrụ ya n'ime ngalaba a na ọtụtụ ụlọ ọrụ, gụnyere South Tees Hosp NHS Fdn Trust, James Cook University Hospital, Royal Cornwall Hospital, Mahadum Sheffield, na Chesterfield Royal Hosp. E wezụga ọkachamara ya na Dermatology Allergy, Cousen, P's research mmasị na ihe omume nwere ike gbasaa na mpaghara ndị yiri ya dị ka ọgwụ mgbochi ọrịa, nyere njikọ dị n'etiti mmeghachi omume nfụkasị na usoro ahụ ji alụso ọrịa ọgụ. Nke a nwere ike ịgụnye ịmụ ihe nzaghachi mgbochi ọrịa na-eduga n'ọnọdụ anụ ahụ nfụkasị na ịchọpụta ụzọ ọgwụgwọ ọhụrụ iji gbanwee azịza ndị a.
Na mgbakwunye, nyocha ya nwere ike ịgụnye nnwale ụlọ ọgwụ maka ọgwụgwọ dermatological ọhụrụ, nyocha ọrụ mgbochi akpụkpọ ahụ na ọrụ ọ na-eme na mgbochi nke nrịanrịa, na nyocha nke mkpụrụ ndụ ihe nketa na-ebunye ndị mmadụ n'otu n'otu na allergies akpụkpọ ahụ. Ọzọkwa, n'ịtụle ọdịdị dị iche iche nke nyocha ahụike ahụike, ọ nwere ike iso ndị ọkachamara sitere na mpaghara ndị ọzọ dị ka ọgwụ ọgwụ, microbiology (na-amụ mmetụta microbiome akpụkpọ anụ na allergies), na ọbụna nkà mmụta uche (na-enyocha mmetụta uche nke ọrịa anụ ahụ na-adịghị ala ala), si otú a na-enye aka na nghọta zuru oke na njikwa nke ọnọdụ nrịanrịa dermatological. Cousen, P na-edepụtara na ntụaka nke ntụaka [4].
