CCK-4

Izvor: Wikipedia
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]

Vidi još[uredi - уреди]

Reference[uredi - уреди]

  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". Neuropsychopharmacology 30 (1): 192–195. doi:10.1038/sj.npp.1300572. PMID 15467707. 
  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. doi:10.1016/j.neuroimage.2006.01.035. PMID 16600640. 
  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. doi:10.1007/s00213-007-0738-7. PMID 17318504. 
  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. doi:10.1002/hbm.20522. PMID 18095276. 
  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. doi:10.1016/0167-0115(82)90080-5. PMID 6291099. 
  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. doi:10.1021/jm9603072. PMID 9057851. 
  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. doi:10.1021/jm0000416. PMID 11020275. 
  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. doi:10.1007/s002130000517. PMID 11205416. 
  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. doi:10.1016/S0223-5234(03)00112-0. PMID 12932898. 
  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. doi:10.1007/s00210-004-0969-7. PMID 15480577. 
  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. doi:10.1021/jm050921q. PMC 1484468. PMID 16686530. 
  15. Noble F (2007). "Pharmacology of CCKRs and SAR studies of peptidic analog ligands". Current Topics in Medicinal Chemistry 7 (12): 1173–9. doi:10.2174/156802607780960447. PMID 17584139. 
  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. doi:10.2174/156802607780960537. PMID 17584140. 
  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. doi:10.2174/156802607780960500. PMID 17584141. 

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