By Cocer Peptides 
1 ọnwa gara aga
Edemede na ozi ngwaahịa niile enyere na webụsaịtị a bụ naanị maka mgbasa ozi na ebumnuche mmụta.
Ngwaahịa ndị enyere na webụsaịtị a bụ naanị maka nyocha in vitro. A na-eme nyocha in vitro (Latin: * na iko *, nke pụtara na ihe eji enyo) na mpụga ahụ mmadụ. Ngwaahịa ndị a abụghị ọgwụ, ndị US Food and Drug Administration (FDA) akwadoghị ya, ha agaghịkwa eji ya gbochie, gwọọ, ma ọ bụ gwọọ ọnọdụ ahụike ọ bụla, ọrịa, ma ọ bụ ọrịa. Iwu amachibidoro nke ọma iwebata ngwaahịa ndị a n'ime ahụ mmadụ ma ọ bụ anụmanụ n'ụdị ọ bụla.
Dermorphin bụ peptide opioid nwere ike dịpụrụ adịpụ na akpụkpọ nke ụfọdụ ụdị frog.
Usoro nke mmetụta analgesic nke Dermorphin
Mmekọrịta ya na ndị na-anabata Opioid
Dermorphin na-arụ ọrụ mmetụta analgesic ya site na mmekọrịta ya na onye na-anabata μ-opioid (MOP). Onye na-anabata μ-opioid bụ onye bụ isi nke ezinụlọ nnabata opioid ma na-arụ ọrụ dị mkpa na mgbanwe mgbu. Dermorphin na analogues ya nwere ike jikọta kpọmkwem na onye na-anabata MOP, dị ka igodo dabara na mkpọchi, si otú a na-eme ka ụzọ mgbama mgbada na-agbada. [Cys (ATTO 488) 8] Dermorphin - NH₂ (DermATTO488), akwụkwọ akụkọ fluorescent Dermorphin analog nke dabeere na ATTO488, na-ejikọta na sel HEK na CHO na-egosipụta ndị na-anabata MOP mmadụ ma na-egosipụta njirimara njide yiri nke Dermorphin. Ọ na-akpali njikọ protein G, na-akwalite njikọ GTPγ[35S], si otú a na-eme ka ntụgharị mgbaàmà metụtara ya, na n'ikpeazụ na-egbochi nnyefe mgbaàmà mgbu. Dermorphin na-akpalikwa ERK1 / 2 phosphorylation, na-enwekwu mmetụta na usoro ndu intracellular ma na-ekere òkè na nhazi nke mmetụta analgesic.
Mgbochi nke nnyefe mgbaàmà mgbu na ọkwa ọkpụkpụ azụ
Nnyocha nyocha egosila na Dermorphin na-egbochi nrịanrịa mgbaàmà mgbu na ọkwa ọkpụkpụ azụ. N'ime nnwale, infusion intravenous nke 0.16 mg / kg Dermorphin mere ka mmụba dị ịrịba ama na nke na-adịgide adịgide na nociceptive flexion reflex threshold na ndị ọrụ afọ ofufo dị mma, a na-ekwupụtakwa mmetụta a na ndị nwere mmerụ ahụ na-adịghị ala ala, na-egosi na Dermorphin bụ isi na-egbochi nnyefe nociceptive na ọkwa ọkpụkpụ azụ. Usoro a na-eme nwere ike ịmetụta usoro Dermorphin nke ntọhapụ neurotransmitter n'ime ọkpụkpụ azụ ma ọ bụ ihe ọ na-eme kpọmkwem na akwara ọkpụkpụ azụ. Ọkpụkpụ azụ na-eje ozi dị ka ebe dị mkpa maka nnyefe mgbaàmà mgbu, na nhazi nke Dermorphin nke ọrụ ya na-egbochi nnyefe elu nke mgbaàmà mgbu na ụbụrụ, si otú ahụ nweta mmetụta analgesic.
Njirimara omume nnabata pụrụ iche
Ọ bụ ezie na naloxone nwere ike imegide mmetụta nke morphine na analogs nke opioid kpamkpam, ọ nwere ike ịmegharị naanị ihe mgbochi nke Dermorphin na ntụgharị azụ azụ nociceptive. Nke a na-egosi na Dermorphin na-emekọrịta ihe na otu dị iche iche nke ndị na-anabata opioid spinal mgbe ọ na-ebute analgesia, na usoro ya dị iche na nke ọgwụ opioid omenala. Ụdị omume a na-enye ụfọdụ uru na ngwa analgesic, dị ka ibelata mmetụta ndị a na-ahụkarị metụtara ọgwụ opioid ọdịnala.
Ọrụ analgesic nke Dermorphin na nnwale anụmanụ
Analgesia dị irè n'ụdị anụmanụ ọtụtụ
N'ụdị mgbu anụmanụ dị iche iche, Dermorphin gosipụtara mmetụta analgesic dị ike. N'ime nnwale ndị dị ka ọdụ-flick, efere ọkụ, ntụtụ ọdụ, formalin, na acetic acid writhing ule, intraperitoneal nchịkwa nke Dermorphin na ya metụtara peptides belatara ụmụ anụmanụ mmetụta na mgbu na mụbaa ha mgbu ọnụ ụzọ. Nnwale ndị a gosipụtara mgbu nke ogo na ụdị dị iche iche, na-akwado ike nke analgesic Dermorphin. N'ime ule a na-ekpo ọkụ na-ekpo ọkụ, mgbe o nyechara Dermorphin n'anụmanụ, oge nkwụsị maka ịracha ụkwụ ha ma ọ bụ ịwụ elu na-agbatị ogologo oge, na-egosi nzaghachi mgbu na-adịghị ike na mkpali okpomọkụ, si otú ahụ na-egosipụta mmetụta analgesic nke Dermorphin dị mma.
Uru Ntụnyere N'ọgwụgwọ Ọrịa Analgesic Ndị Ọzọ
Tụnyere ọgwụ analgesic ọdịnala dị ka morphine, Dermorphin na-egosipụta uru dị ukwuu na akụkụ ụfọdụ. N'ụdị anụmanụ, mgbe nchịkwa intracerebroventricular gasịrị, Dermorphin gosipụtara mmetụta analgesic nhọrọ na ike karịa morphine, yana ogologo oge nke ime ihe. Ụfọdụ synthesized Dermorphin tetrapepetides gosikwara ọrụ analgesic dị elu, na-enwe ike mgbakasị ahụ ihe dịka ugboro 1,500 na ugboro 17 nke morphine mgbe nchịkwa intracerebroventricular ma ọ bụ subcutaneous na ụmụ oke, n'otu n'otu. Uru ndị a na-enye atụmanya na-atụ anya maka ngwa ụlọ ọgwụ nke Dermorphin na analgesia, nwere ike na-ekwu maka adịghị ike nke ọgwụ analgesic ọdịnala, dị ka ezughị ezu analgesic nrụpụta ma ọ bụ ogologo oge.
Nnyocha na ngwa nyocha nke Dermorphin n'ime mmadụ
Nsonaazụ nnwale ụlọọgwụ mbụ
N'afọ 1985, nnwale ụlọ ọgwụ a na-achịkwaghị achịkwa, ebe a na-achịkwa ebebo na iji Dermorphin maka mgbu na-aga n'ihu gosipụtara na Dermorphin nke a na-enye site na intrathecal injections pụtara ìhè nke ọma placebo na morphine (eji dị ka ihe ntinye aka) n'ihe gbasara ịdị irè nke analgesic. Ihe omumu ihe omumu a nyere ihe akaebe nkwado siri ike maka ngwa ọgwụgwọ nke Dermorphin na analgesia, na-egosipụta ike ya dị ukwuu na nlekọta mgbu mgbe ọ gasịrị.
Ọnọdụ Ngwa enwere ike
Nlekọta mgbu na-aga n'ihu: Ọrịa ịwa ahụ nwere ike ime ka mgbu na-egbu mgbu gasịrị, na-emetụta mgbake nke ndị ọrịa na ịdị mma nke ndụ. Deremorphin gosipụtara ịdị irè n'ibelata mgbu mgbe ịwachara ahụ n'oge ule ụlọ ọgwụ n'oge na-etinye ya dị ka nhọrọ ọhụrụ na-ekwe nkwa maka analgesia postoperative. Tụnyere ọgwụ analgesic ọdịnala mgbe arụchara ọrụ gasịrị, usoro omume ya pụrụ iche na uru ya—dị ka mbelata ihe ize ndụ nke nnabata ọgwụ na ịdabere na ya—na-enye ndị ọrịa ọgwụgwọ analgesic dị mma ma dịkwa irè karị.
Ọgwụgwọ mgbu na-adịghị ala ala: Maka ndị ọrịa nwere ihe mgbu na-adịghị ala ala, karịsịa ndị na-enweghi nzaghachi na-adịghị mma maka ọgwụ analgesic ọdịnala ma ọ bụ nwee mmetụta dị ịrịba ama, Dermorphin nwere ike ịbụ nhọrọ ọgwụgwọ ọzọ bara uru. Na njikwa nke mgbu na-adịghị ala ala na ndị ọrịa cancer, usoro ọgwụgwọ ugbu a ka nwere ụfọdụ njedebe. Mpụta nke Dermorphin na-ewetara ndị ọrịa a olileanya ọhụrụ. Mmetụta analgesic ya na-adịte aka nwere ike ịchịkwa mgbu na-adịgide adịgide na ndị ọrịa cancer ma melite ogo ndụ ha.
Nlebara anya nke palliative: Na ntọala nlekọta palliative, ibelata ihe mgbu nke ndị ọrịa bụ ihe kacha mkpa. Ngwongwo analgesic nke Dermorphin na-eme ka ọ bụrụ onye na-ekwe nkwa ibelata ihe mgbu na njedebe nke ndụ na nlekọta palliative. Site na usoro nchịkwa kwesịrị ekwesị na mgbanwe dose, ọ nwere ike inyere ndị ọrịa aka ibelata nhụjuanya ma welie nkasi obi n'oge ikpeazụ nke ndụ.
Mmechi
Dị ka ihe nwere usoro analgesic pụrụ iche na mmetụta analgesic dị ịrịba ama, Dermorphin na-ejide ngwa ndị na-ekwe nkwa na mpaghara nchịkwa mgbu.
Isi mmalite
[1] Giakomidi D, Bird MF, McDonald J, et al. Nyocha nke [Cys (ATTO 488) 8] Dermorphin-NH2 dị ka ngwá ọrụ ọhụrụ maka ọmụmụ nke μ-opioid peptide receptors[J]. Plos Otu, 2021,16 (4): e250011.DOI:10.1371/journal.pone.0250011.
[2] Hesselink J, Schatman, M E. Nchọpụta ọgwụ ochie: ihe echefuru echefu nke dermorphin maka mgbu na mgbu na-esote [J]. Akwụkwọ akụkọ nyocha ihe mgbu, 2018,11:2991-2995.DOI:10.2147/JPR.S186082.
[3] Guzevatykh LS, Voronina TA, Emel'Ianova TG, et al. Ntụle nyocha nke ọrụ analgesic nke dermorphin, [DPro6] -dermorphin, na C-terminal tripeptides [J]. Izv Akad Nauk Ser Biol, 2007 (5): 577-582. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=18038625&query_hl=1
[4] Sandrini G, Degli UE, Salvadori S, et al. Dermorphin na-egbochi ntugharị azụ azụ nociceptive n'ime mmadụ [J]. Nyocha ụbụrụ, 1986,371 (2): 364-367.DOI: 10.1016 / 0006-8993 (86) 90376-8.
[5] Salvadori S, Marastoni M, Balboni G, et al. Synthesis na opioid ọrụ nke dermorphin tetrapeptides na-ebu D-methionine S-oxide na ọnọdụ 2[J]. Akwụkwọ akụkọ nke ọgwụ Chemistry, 1986,29 (6): 889-894.DOI: 10.1021 / jm00156a003.
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