Википедија

MK-677

MK-677 (L-163,191) je lek koji deluje kao potentan1, oralno aktivan izlučivač hormona rasta.[1][2] On oponaša GH stimulišuće dejstvo endogenog hormona grelina.[3][4] Pokazano je da povišava oslobađanje i održava povišene nivoe u plazmi nekoliko hormona među kojima su hormon rasta i IGF-1, i da nema uticaje na nivoe kortizola.[5]

MK-677
IUPAC ime
1'-(2-metilalanil-O-benzil-D-seril)-1-(metilsulfonil)-1,2-dihidrospiro[indol-3,4'-piperidin]
Identifikatori
PubChemCID 9939050
Sinonimi2-Amino-2-metil-N-[1-(1-metilsulfonilspiro[2H-indol-3,4'-piperidin]-1'-il)-1-okso-3-(fenilmetoksi)propan-2-il]propanamid
Hemijski podaci
FormulaC27H36N4O5S
Molarna masa528,662 g/mol
  • O=S(C)(=O)N(C2)c1ccccc1C23CCN(CC3)C(=O)C(NC(=O)C(N)(C)C)COCc4ccccc4

On je trenutno u razvoju kao potencijalni tretman za redukciju nivoa tih hormona, kao što je nedostatak hormona rasta kod dece ili starijih odraslih osoba.[6][7][8] Klinička ispitivanja su pokazala da povećava mišićnu masu i gustinu minerala kostiju,[9][10] što ga potencijalno čini podesnim za lečenje slabosti starijih osoba.[11][12] On takođe menja metabolizam telesne masnoće tako da možda može da nađe primenu u lečenju gojaznosti.[13][14]

Vidi još уреди

Reference уреди

  1. ^ Patchett, A. A.; Nargund, R. P.; Tata, J. R.; Chen, M. H.; Barakat, K. J.; Johnston, D. B.; Cheng, K.; Chan, W. W.; Butler, B.; Hickey, G.; Jacks, T.; Schleim, K.; Pong, S. -S.; Chaung, L. -Y. P.; Chen, H. Y.; Frazier, E.; Leung, K. H.; Chiu, S. -H. L.; Smith, Roy G. (1995). „Design and biological activities of L-163,191 (MK-0677): A potent, orally active growth hormone secretagogue”. Proceedings of the National Academy of Sciences of the United States of America. 7624358 (15): 7001—7005. Bibcode:1995PNAS...92.7001P. PMC 41459  . PMID 7624358. doi:10.1073/pnas.92.15.7001  . 
  2. ^ Pong, S. S.; Chaung, L. Y.; Dean, D. C.; Nargund, R. P.; Patchett, A. A.; Smith, R. G. (1996). „Identification of a new G-protein-linked receptor for growth hormone secretagogues”. Molecular Endocrinology (Baltimore, Md.). 8838145 (1): 57—61. PMID 8838145. doi:10.1210/mend.10.1.8838145. 
  3. ^ Cassoni, P.; Papotti, M.; Ghè, C.; Catapano, F.; Sapino, A.; Graziani, A.; Deghenghi, R.; Reissmann, T.; Ghigo, E.; Muccioli, G. (2001). „Identification, characterization, and biological activity of specific receptors for natural (Ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines”. The Journal of Clinical Endocrinology and Metabolism. 11297611 (4): 1738—1745. PMID 11297611. doi:10.1210/jcem.86.4.7402. 
  4. ^ Holst, B.; Frimurer, T. M.; Mokrosinski, J.; Halkjaer, T.; Cullberg, K. B.; Underwood, C. R.; Schwartz, T. W. (2009). „Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor”. Molecular Pharmacology. 18923064 (1): 44—59. PMID 18923064. S2CID 2218638. doi:10.1124/mol.108.049189. 
  5. ^ Copinschi, G.; Van Onderbergen, A.; l'Hermite-Balériaux, M.; Mendel, C. M.; Caufriez, A.; Leproult, R.; Bolognese, J. A.; De Smet, M.; Thorner, M. O.; Van Cauter, E. (1996). „Effects of a 7-day treatment with a novel, orally active, growth hormone (GH) secretagogue, MK-677, on 24-hour GH profiles, insulin-like growth factor I, and adrenocortical function in normal young men”. The Journal of Clinical Endocrinology and Metabolism. 8768828 (8): 2776—2782. PMID 8768828. doi:10.1210/jcem.81.8.8768828. 
  6. ^ Chapman, I. M.; Bach, M. A.; Van Cauter, E.; Farmer, M.; Krupa, D.; Taylor, A. M.; Schilling, L. M.; Cole, K. Y.; Skiles, E. H.; Pezzoli, S. S.; Hartman, M. L.; Veldhuis, J. D.; Gormley, G. J.; Thorner, M. O. (1996). „Stimulation of the growth hormone (GH)-insulin-like growth factor I axis by daily oral administration of a GH secretogogue (MK-677) in healthy elderly subjects”. The Journal of Clinical Endocrinology and Metabolism. 8954023 (12): 4249—4257. PMID 8954023. doi:10.1210/jcem.81.12.8954023. 
  7. ^ Thorner, M. O.; Chapman, I. M.; Gaylinn, B. D.; Pezzoli, S. S.; Hartman, M. L. (1997). „Growth hormone-releasing hormone and growth hormone-releasing peptide as therapeutic agents to enhance growth hormone secretion in disease and aging”. Recent Progress in Hormone Research. 9238854: 215—44; discussion 244—6. PMID 9238854. 
  8. ^ Chapman, I. M.; Pescovitz, O. H.; Murphy, G.; Treep, T.; Cerchio, K. A.; Krupa, D.; Gertz, B.; Polvino, W. J.; Skiles, E. H.; Pezzoli, S. S.; Thorner, M. O. (1997). „Oral administration of growth hormone (GH) releasing peptide-mimetic MK-677 stimulates the GH/Insulin-like growth factor-I axis in selected GH-deficient adults”. The Journal of Clinical Endocrinology and Metabolism. 9329386 (10): 3455—3463. PMID 9329386. doi:10.1210/jcem.82.10.4297. 
  9. ^ Murphy, M. G.; Bach, M. A.; Plotkin, D.; Bolognese, J.; Ng, J.; Krupa, D.; Cerchio, K.; Gertz, B. J. (1999). „Oral administration of the growth hormone secretagogue MK-677 increases markers of bone turnover in healthy and functionally impaired elderly adults. The MK-677 Study Group”. Journal of Bone and Mineral Research : The Official Journal of the American Society for Bone and Mineral Research. 10404019 (7): 1182—1188. PMID 10404019. S2CID 44368393. doi:10.1359/jbmr.1999.14.7.1182. 
  10. ^ Murphy, M. G.; Weiss, S.; McClung, M.; Schnitzer, T.; Cerchio, K.; Connor, J.; Krupa, D.; Gertz, B. J.; MK-677/Alendronate Study Group (2001). „Effect of alendronate and MK-677 (A growth hormone secretagogue), individually and in combination, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women”. The Journal of Clinical Endocrinology and Metabolism. 11238495 (3): 1116—1125. PMID 11238495. doi:10.1210/jcem.86.3.7294. 
  11. ^ Smith, R. G.; Sun, Y.; Jiang, H.; Albarran-Zeckler, R.; Timchenko, N. (2007). „Ghrelin receptor (GHS-R1A) agonists show potential as interventive agents during aging”. Annals of the New York Academy of Sciences. 18056963 (1): 147—164. Bibcode:2007NYASA1119..147S. PMID 18056963. S2CID 3220799. doi:10.1196/annals.1404.023. 
  12. ^ „An Anti-frailty Pill For Seniors? New Drug Increases Muscle Mass In Arms And Legs Of Older Adults”. ScienceDaily. 2008. 
  13. ^ Svensson, J.; Lönn, L.; Jansson, J. O.; Murphy, G.; Wyss, D.; Krupa, D.; Cerchio, K.; Polvino, W.; Gertz, B.; Boseaus, I.; Sjöström, L.; Bengtsson, B. A. (1998). „Two-month treatment of obese subjects with the oral growth hormone (GH) secretagogue MK-677 increases GH secretion, fat-free mass, and energy expenditure”. The Journal of Clinical Endocrinology and Metabolism. 9467542 (2): 362—369. PMID 9467542. doi:10.1210/jcem.83.2.4539. 
  14. ^ Svensson, J.; Jansson, J. O.; Ottosson, M.; Johannsson, G.; Taskinen, M. R.; Wiklund, O.; Bengtsson, B. A. (1999). „Treatment of obese subjects with the oral growth hormone secretagogue MK-677 affects serum concentrations of several lipoproteins, but not lipoprotein(a)”. The Journal of Clinical Endocrinology and Metabolism. 10372705 (6): 2028—2033. PMID 10372705. S2CID 24550203. doi:10.1210/jcem.84.6.5799. 


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