| 词条 | Zyklophin |
| 释义 |
| image = Zyklophin.svg | width = 250 | IUPAC_name = N-Benzyl-L-tyrosylglycylglycyl-N-[(3S,6S,9S,12S)-6-[(2S)-2-butanyl]-3-({(2S)-5-carbamimidamido-1-[(2S)-2[(2S)-1,6-diamino-1-oxo-2-hexanyl]carbamoyl1-pyrrolidinyl]-1-oxo-2-pentanyl}carbamoyl)-9-(3-carbamimidamidopropyl)-5,8,11,14-tetraoxo-1,4,7,10-tetraazacyclotetradecan-12-yl]-L-phenylalaninamide | CAS_number = | ATC_prefix = None | ATC_suffix = | PubChem = 45483651 | DrugBank = | ChemSpiderID = 30844961 | C=65 | H=96 | N=20 | O=13 | molecular_weight = 1365.584 g/mol | smiles = CC[C@H](C)[C@H]1C(=O)N[C@@H](CNC(=O)C[C@@H](C(=O)N[C@H](C(=O)N1)CCCNC(=N)N)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)CNC(=O)CNC(=O)[C@H](CC3=CC=C(C=C3)O)NCC4=CC=CC=C4)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N5CCC[C@H]5C(=O)N[C@@H](CCCCN)C(=O)N | StdInChI = 1S/C65H96N20O13/c1-3-38(2)54-62(97)83-49(60(95)81-45(21-13-29-73-65(70)71)63(98)85-30-14-22-50(85)61(96)79-43(55(67)90)19-10-11-27-66)35-75-51(87)33-48(59(94)80-44(57(92)84-54)20-12-28-72-64(68)69)82-58(93)47(32-39-15-6-4-7-16-39)78-53(89)37-76-52(88)36-77-56(91)46(31-40-23-25-42(86)26-24-40)74-34-41-17-8-5-9-18-41/h4-9,15-18,23-26,38,43-50,54,74,86H,3,10-14,19-22,27-37,66H2,1-2H3,(H2,67,90)(H,75,87)(H,76,88)(H,77,91)(H,78,89)(H,79,96)(H,80,94)(H,81,95)(H,82,93)(H,83,97)(H,84,92)(H4,68,69,72)(H4,70,71,73)/t38-,43-,44-,45-,46-,47-,48-,49-,50-,54-/m0/s1 | StdInChIKey = UWLIKQFWZOPOAX-KLROISQLSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Legal | routes_of_administration = }} Zyklophin is a semisynthetic peptide derived from dynorphin A and a highly selective antagonist of the κ-opioid receptor (KOR).[1][2] It is systemically-active, displaying good metabolic stability and blood-brain-barrier penetration.[2] Similarly to other KOR antagonists, it has been shown to block stress-induced reinstatement of cocaine-seeking in animals.[2] The drug is currently experimental, and thus cannot be considered safe for consumption or usage. See also
References1. ^{{cite journal |vauthors=Patkar KA, Yan X, Murray TF, Aldrich JV | title = [Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist | journal = J. Med. Chem. | volume = 48 | issue = 14 | pages = 4500–3 |date=July 2005 | pmid = 15999987 | doi = 10.1021/jm050105i | url = }} {{Opioidergics}}{{nervous-system-drug-stub}}2. ^1 2 {{cite journal |vauthors=Aldrich JV, Patkar KA, McLaughlin JP | title = Zyklophin, a systemically active selective kappa opioid receptor peptide antagonist with short duration of action | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 106 | issue = 43 | pages = 18396–401 |date=October 2009 | pmid = 19841255 | pmc = 2775281 | doi = 10.1073/pnas.0910180106 | url = }} 3 : Kappa antagonists|Opioid peptides|Semisynthetic opioids |
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