CCK-4

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CCK-4
(IUPAC) ime
(3S)-3-[(2S)-2-amino-3-phenylpropanamido]-3[(1S)-1[(1S)-1-carboxy -2-(indol-3-yl)ethyl]carbamoyl3-(methylsulfanyl)propyl]carbamoyl}propanoic acid
Klinički podaci
Identifikatori
CAS broj 1947-37-1
ATC kod  ?
Hemijski podaci
Formula C29H35N5O7S 
Mol. masa 597.681 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 100%
Metabolizam proteaze plazme
Poluvreme eliminacije 13 minuta
Izlučivanje N/A
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status
Način primene 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]

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Reference[uredi - уреди | uredi izvor]

  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. (July 1993). "Neurobiological investigations into the role of cholecystokinin in panic disorder". Journal of Psychiatry and Neuroscience 18 (4): 178–188. PMC 1188527. PMID 8104032. 
  3. ↑ Schunck T, Erb G, Mathis A, Gilles C, Namer IJ, Hode Y, Demaziere A, Luthringer R, Macher JP. (July 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. 
  4. ↑ Eser D, Schüle C, Baghai T, Floesser A, Krebs-Brown A, Enunwa M, de la Motte S, Engel R, Kucher K, Rupprecht R. (July 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. 
  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. (December 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. 
  6. ↑ Koulischer D, Moroder L, Deschodt-Lanckman M (August 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. 
  7. ↑ Blommaert AG, Dhôtel H, Ducos B, Durieux C, Goudreau N, Bado A, Garbay C, Roques BP (February 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. 
  8. ↑ Bellier B, Million ME, DaNascimento S, Meudal H, Kellou S, Maigret B, Garbay C (October 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. 
  9. ↑ Léna I, Dh tel H, Garbay C, Daugé V (January 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. 
  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 (November 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. 
  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 (in Russian) 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 (in Russian) 32 (3): 276–83. PMID 16808170. 
  14. ↑ Agnes RS, Lee YS, Davis P, Ma SW, Badghisi H, Porreca F, Lai J, Hruby VJ (May 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 1484468. PMID 16686530. doi:10.1021/jm050921q. 
  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. 

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