CCK-4 — разлика између измена

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| doi = 10.1016/j.neuroimage.2006.01.035}}</ref><ref>{{Cite journal | author = Eser D, Schüle C, Baghai T, Floesser A, Krebs-Brown A, Enunwa M, de la Motte S, Engel R, Kucher K, Rupprecht R. | title = Evaluation of the CCK-4 model as a challenge paradigm in a population of healthy volunteers within a proof-of-concept study | journal = Psychopharmacology | year = 2007 | month = July | volume = 192 | issue = 4 | pages = 479–487 | pmid = 17318504 | doi = 10.1007/s00213-007-0738-7}}</ref><ref>{{Cite journal | author = Eser D, Leicht G, Lutz J, Wenninger S, Kirsch V, Schüle C, Karch S, Baghai T, Pogarell O, Born C, Rupprecht R, Mulert C. | title = Functional neuroanatomy of CCK-4-induced panic attacks in healthy volunteers | journal = Human Brain Mapping | year = 2007
| doi = 10.1016/j.neuroimage.2006.01.035}}</ref><ref>{{Cite journal | author = Eser D, Schüle C, Baghai T, Floesser A, Krebs-Brown A, Enunwa M, de la Motte S, Engel R, Kucher K, Rupprecht R. | title = Evaluation of the CCK-4 model as a challenge paradigm in a population of healthy volunteers within a proof-of-concept study | journal = Psychopharmacology | year = 2007 | month = July | volume = 192 | issue = 4 | pages = 479–487 | pmid = 17318504 | doi = 10.1007/s00213-007-0738-7}}</ref><ref>{{Cite journal | author = Eser D, Leicht G, Lutz J, Wenninger S, Kirsch V, Schüle C, Karch S, Baghai T, Pogarell O, Born C, Rupprecht R, Mulert C. | title = Functional neuroanatomy of CCK-4-induced panic attacks in healthy volunteers | journal = Human Brain Mapping | year = 2007
| month = December | pmid = 18095276 | volume = 30 | issue = 2 | pages = 511–22 | doi = 10.1002/hbm.20522}}</ref>
| month = December | pmid = 18095276 | volume = 30 | issue = 2 | pages = 511–22 | doi = 10.1002/hbm.20522}}</ref>

Pošto je on peptid, -{CCK-4}- mora biti administriran putem injekcije. U telu se brzo razlaže, tako da ima kratkotrajno dejstvo.<ref>{{Cite journal | author = Koulischer D, Moroder L, Deschodt-Lanckman M | title = Degradation of cholecystokinin octapeptide, related fragments and analogs by human and rat plasma in vitro | journal = Regulatory Peptides | year = 1982 | month = August | volume = 4 | issue = 3 | pages = 127–139 | pmid = 6291099
| doi = 10.1016/0167-0115(82)90080-5}}</ref> Brojni sintetički analozi sa modifikovanim osobinama su poznati.<ref name="pmid9057851">{{cite journal |author=Blommaert AG, Dhôtel H, Ducos B, Durieux C, Goudreau N, Bado A, Garbay C, Roques BP |title=Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor |journal=Journal of Medicinal Chemistry |volume=40 |issue=5 |pages=647–58 |year=1997 |month=February |pmid=9057851 |doi=10.1021/jm9603072 |url=}}</ref><ref name="pmid11020275">{{cite journal |author=Bellier B, Million ME, DaNascimento S, Meudal H, Kellou S, Maigret B, Garbay C |title=Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode |journal=Journal of Medicinal Chemistry |volume=43 |issue=20 |pages=3614–23 |year=2000 |month=October |pmid=11020275 |doi= 10.1021/jm0000416|url=}}</ref><ref name="pmid11205416">{{cite journal |author=Léna I, Dh tel H, Garbay C, Daugé V |title=Involvement of D2 dopamine receptors in the opposing effects of two CCK-B agonists in a spatial recognition memory task: role of the anterior nucleus accumbens |journal=Psychopharmacology |volume=153 |issue=2 |pages=170–9 |year=2001 |month=January |pmid=11205416 |doi= 10.1007/s002130000517|url=}}</ref><ref name="pmid12932898">{{cite journal |author=Bellier B, Garbay C |title=How a single inversion of configuration leads to a reversal of the binding mode: proposal of a novel arrangement of CCK2 ligands in their receptor, and contribution to the development of peptidomimetic or non-peptide CCK2 ligands |journal=European Journal of Medicinal Chemistry |volume=38 |issue=7-8 |pages=671–86 |year=2003 |pmid=12932898 |doi= 10.1016/S0223-5234(03)00112-0|url=}}</ref><ref name="pmid15480577">{{cite journal |author=Bellier B, Crété D, Million ME, Beslot F, Bado A, Garbay C, Daugé V |title=New CCK2 agonists confirming the heterogeneity of CCK2 receptors: characterisation of BBL454 |journal=Naunyn-Schmiedeberg's Archives of Pharmacology |volume=370 |issue=5 |pages=404–13 |year=2004 |month=November |pmid=15480577 |doi=10.1007/s00210-004-0969-7 |url=}}</ref><ref name="pmid15889786">{{cite journal |author=Proskuriakova TV, Bespalova ZhD, Pal'keeva ME, Petrichenko OB, Pankratova NV, Shokhonova VA, Anokhina IP |title=[Biological activity of cholecystokinin-(30-33) tetrapeptide analogs] |language=Russian |journal=Bioorganicheskaia Khimiia |volume=31 |issue=2 |pages=130–9 |year=2005 |pmid=15889786 |doi= |url=}}</ref><ref name="pmid16808170">{{cite journal |author=Anokhina IP, Proskuriakova TV, Bespalova ZhD, Pal'keeva ME, Shokhonova VA, Petrichenko OB |title=[Effect of a cholecystokinin tetrapeptide analogue on opioid reception under acute and chronic morphine administration] |language=Russian |journal=Bioorganicheskaia Khimiia |volume=32 |issue=3 |pages=276–83 |year=2006 |pmid=16808170 |doi= |url=}}</ref><ref name="pmid16686530">{{cite journal |author=Agnes RS, Lee YS, Davis P, Ma SW, Badghisi H, Porreca F, Lai J, Hruby VJ |title=Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors |journal=Journal of Medicinal Chemistry |volume=49 |issue=10 |pages=2868–75 |year=2006 |month=May |pmid=16686530 |pmc=1484468 |doi=10.1021/jm050921q |url=}}</ref><ref name="pmid17584139">{{cite journal |author=Noble F |title=Pharmacology of CCKRs and SAR studies of peptidic analog ligands |journal=Current Topics in Medicinal Chemistry |volume=7 |issue=12 |pages=1173–9 |year=2007 |pmid=17584139 |doi= 10.2174/156802607780960447|url=}}</ref><ref name="pmid17584140">{{cite journal |author=García-López MT, González-Muñiz R, Martín-Martínez M, Herranz R |title=Strategies for design of non peptide CCK1R agonist/antagonist ligands |journal=Current Topics in Medicinal Chemistry |volume=7 |issue=12 |pages=1180–94 |year=2007 |pmid=17584140 |doi= 10.2174/156802607780960537|url=}}</ref><ref name="pmid17584141">{{cite journal |author=Kalindjian SB, McDonald IM |title=Strategies for the design of non-peptide CCK2 receptor agonist and antagonist ligand |journal=Current Topics in Medicinal Chemistry |volume=7 |issue=12 |pages=1195–204 |year=2007 |pmid=17584141 |doi= 10.2174/156802607780960500|url=}}</ref>


== Literatura ==
== Literatura ==

Верзија на датум 31. мај 2011. у 06:52

{{Drugbox-lat | IUPAC_name = (3S)-3-[(2S)-2-amino-3-phenylpropanamido]-3-{[(1S)-1[(1S)-1-carboxy -2-(indol-3-yl)ethyl]carbamoyl3-(methylsulfanyl)propyl]carbamoyl}propanoic acid | image = CCK-4.png | width = 240 | CAS_number = 1947-37-1 | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank = | C=29|H=35|N=5|O=7|S=1 | molecular_weight = 597.681 g/mol | smiles = c3cccc1c3ncc1CC(C(=O)O)NC(=O)C(CCSC)NC(=O)C(CC(O)=O)NC(=O)C(N)Cc2ccccc2 | bioavailability = 100% | protein_bound = | metabolism = proteaze plazme | elimination_half-life = 13 minuta | excretion = N/A | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = IV }}

CCK-4 (holecistokininski tetrapeptid, Trp-Met-Asp-Phe-NH2; ili PTK7) je peptidni fragment izveden iz većeg peptidnog hormona holecistokinina. Za razliku od holecistokina koji ima niz uloga u gastrointestinalnom sistemu kao i u centralnom nervnom sistemu, CCK-4 deluje prvenstveno u mozgu kao stimulator anksioznosti. On pokazuje slabe GI efekte, za razliku od CCK-8 ili polipeptida pune dužine, CCK-58.

CCK-4 proizvodi jake simptome anksioznosti u malim dozama, kao što je 50 μg,[1] i često se koristi u naučnim istraživanjima za indukovanje paničnih napada s ciljem testiranja novih anksiolitika.[2][3][4][5]

Pošto je on peptid, CCK-4 mora biti administriran putem injekcije. U telu se brzo razlaže, tako da ima kratkotrajno dejstvo.[6] Brojni sintetički analozi sa modifikovanim osobinama su poznati.[7][8][9][10][11][12][13][14][15][16][17]

Literatura

  1. ^ Daniela Eser; et al. (2005). „Panic Induction with Cholecystokinin-Tetrapeptide (CCK-4) Increases Plasma Concentrations of the Neuroactive Steroid 3α, 5α Tetrahydrodeoxycorticosterone (3α, 5α-THDOC) in Healthy Volunteers” (PDF). Neuropsychopharmacology. 30 (1): 192—195. PMID 15467707. doi:10.1038/sj.npp.1300572. 
  2. ^ Bradwejn J. (1993). „Neurobiological investigations into the role of cholecystokinin in panic disorder”. Journal of Psychiatry and Neuroscience. 18 (4): 178—188. PMC 1188527Слободан приступ. PMID 8104032.  Непознати параметар |month= игнорисан (помоћ)
  3. ^ Schunck T, Erb G, Mathis A, Gilles C, Namer IJ, Hode Y, Demaziere A, Luthringer R, Macher JP. (2006). „Functional magnetic resonance imaging characterization of CCK-4-induced panic attack and subsequent anticipatory anxiety”. NeuroImage. 31 (3): 1197—1208. PMID 16600640. doi:10.1016/j.neuroimage.2006.01.035.  Непознати параметар |month= игнорисан (помоћ)
  4. ^ Eser D, Schüle C, Baghai T, Floesser A, Krebs-Brown A, Enunwa M, de la Motte S, Engel R, Kucher K, Rupprecht R. (2007). „Evaluation of the CCK-4 model as a challenge paradigm in a population of healthy volunteers within a proof-of-concept study”. Psychopharmacology. 192 (4): 479—487. PMID 17318504. doi:10.1007/s00213-007-0738-7.  Непознати параметар |month= игнорисан (помоћ)
  5. ^ Eser D, Leicht G, Lutz J, Wenninger S, Kirsch V, Schüle C, Karch S, Baghai T, Pogarell O, Born C, Rupprecht R, Mulert C. (2007). „Functional neuroanatomy of CCK-4-induced panic attacks in healthy volunteers”. Human Brain Mapping. 30 (2): 511—22. PMID 18095276. doi:10.1002/hbm.20522.  Непознати параметар |month= игнорисан (помоћ)
  6. ^ Koulischer D, Moroder L, Deschodt-Lanckman M (1982). „Degradation of cholecystokinin octapeptide, related fragments and analogs by human and rat plasma in vitro”. Regulatory Peptides. 4 (3): 127—139. PMID 6291099. doi:10.1016/0167-0115(82)90080-5.  Непознати параметар |month= игнорисан (помоћ)
  7. ^ Blommaert AG, Dhôtel H, Ducos B, Durieux C, Goudreau N, Bado A, Garbay C, Roques BP (1997). „Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor”. Journal of Medicinal Chemistry. 40 (5): 647—58. PMID 9057851. doi:10.1021/jm9603072.  Непознати параметар |month= игнорисан (помоћ)
  8. ^ Bellier B, Million ME, DaNascimento S, Meudal H, Kellou S, Maigret B, Garbay C (2000). „Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode”. Journal of Medicinal Chemistry. 43 (20): 3614—23. PMID 11020275. doi:10.1021/jm0000416.  Непознати параметар |month= игнорисан (помоћ)
  9. ^ Léna I, Dh tel H, Garbay C, Daugé V (2001). „Involvement of D2 dopamine receptors in the opposing effects of two CCK-B agonists in a spatial recognition memory task: role of the anterior nucleus accumbens”. Psychopharmacology. 153 (2): 170—9. PMID 11205416. doi:10.1007/s002130000517.  Непознати параметар |month= игнорисан (помоћ)
  10. ^ Bellier B, Garbay C (2003). „How a single inversion of configuration leads to a reversal of the binding mode: proposal of a novel arrangement of CCK2 ligands in their receptor, and contribution to the development of peptidomimetic or non-peptide CCK2 ligands”. European Journal of Medicinal Chemistry. 38 (7-8): 671—86. PMID 12932898. doi:10.1016/S0223-5234(03)00112-0. 
  11. ^ Bellier B, Crété D, Million ME, Beslot F, Bado A, Garbay C, Daugé V (2004). „New CCK2 agonists confirming the heterogeneity of CCK2 receptors: characterisation of BBL454”. Naunyn-Schmiedeberg's Archives of Pharmacology. 370 (5): 404—13. PMID 15480577. doi:10.1007/s00210-004-0969-7.  Непознати параметар |month= игнорисан (помоћ)
  12. ^ Proskuriakova TV, Bespalova ZhD, Pal'keeva ME, Petrichenko OB, Pankratova NV, Shokhonova VA, Anokhina IP (2005). „[Biological activity of cholecystokinin-(30-33) tetrapeptide analogs]”. Bioorganicheskaia Khimiia (на језику: руски). 31 (2): 130—9. PMID 15889786. 
  13. ^ Anokhina IP, Proskuriakova TV, Bespalova ZhD, Pal'keeva ME, Shokhonova VA, Petrichenko OB (2006). „[Effect of a cholecystokinin tetrapeptide analogue on opioid reception under acute and chronic morphine administration]”. Bioorganicheskaia Khimiia (на језику: руски). 32 (3): 276—83. PMID 16808170. 
  14. ^ Agnes RS, Lee YS, Davis P, Ma SW, Badghisi H, Porreca F, Lai J, Hruby VJ (2006). „Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors”. Journal of Medicinal Chemistry. 49 (10): 2868—75. PMC 1484468Слободан приступ. PMID 16686530. doi:10.1021/jm050921q.  Непознати параметар |month= игнорисан (помоћ)
  15. ^ Noble F (2007). „Pharmacology of CCKRs and SAR studies of peptidic analog ligands”. Current Topics in Medicinal Chemistry. 7 (12): 1173—9. PMID 17584139. doi:10.2174/156802607780960447. 
  16. ^ García-López MT, González-Muñiz R, Martín-Martínez M, Herranz R (2007). „Strategies for design of non peptide CCK1R agonist/antagonist ligands”. Current Topics in Medicinal Chemistry. 7 (12): 1180—94. PMID 17584140. doi:10.2174/156802607780960537. 
  17. ^ Kalindjian SB, McDonald IM (2007). „Strategies for the design of non-peptide CCK2 receptor agonist and antagonist ligand”. Current Topics in Medicinal Chemistry. 7 (12): 1195—204. PMID 17584141. doi:10.2174/156802607780960500.