Takrolimus

Takrolimus
Klinički podaci
Prodajno ime	Advagraf, Hecoria, Prograf, Protopic
Drugs.com	Monografija
Način primene	Oralno, intravenozno, topikalno
Identifikatori
CAS broj	104987-11-3
ATC kod	D11AH01 (WHO), L04AD02
PubChem	CID 445647
DrugBank	DB00864
ChemSpider	4976056
KEGG	C01375
ChEBI	CHEBI:61049
ChEMBL	CHEMBL269732

Takrolimus je organsko jedinjenje, koje sadrži 44 atoma ugljenika i ima molekulsku masu od 804,018 Da.^[1]^[2]^[3]^[4]^[5]^[6]^[7]

Osobine

Osobina	Vrednost
Broj akceptora vodonika	12
Broj donora vodonika	3
Broj rotacionih veza	7
Particioni koeficijent^[8] (ALogP)	4,8
Rastvorljivost^[9] (logS, log(mol/L))	-7,9
Polarna površina^[10] (PSA, Å²)	178,3

Reference

^ Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). . . 40 (9): 1249—55. 1987 Sep. PMID 2445721. Проверите вредност парамет(а)ра за датум: |date= (помоћ); Недостаје или је празан параметар |title= (помоћ)
^ Pritchard DI. . „Sourcing a chemical succession for cyclosporin from parasites and human pathogens”. Drug Discov Today. 10 (10): 688—91. 2005 May 15. PMID 15896681. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL. . „Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes”. Cell. 66 (4): 807—15. 1991 Aug 23. PMID 1715244. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K. . „Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient”. Drug Metab Pharmacokinet. 21 (2): 122—5. 2006 Apr. PMID 16702731. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Hanifin JM, Paller AS, Eichenfield L, Clark RA, Korman N, Weinstein G, Caro I, Jaracz E, Rico MJ: Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis. J Am Acad Dermatol. 2005 Aug;53(2 Suppl 2):S186-94. . . PMID 16021174. Недостаје или је празан параметар |title= (помоћ)
^ Knox, C.; Law, V.; Jewison, T.; Liu, P.; Ly, S.; Frolkis, A.; Pon, A.; Banco, K.; Mak, C.; Neveu, V.; Djoumbou, Y.; Eisner, R.; Guo, A. C.; Wishart, D. S. (2011). . „DrugBank 3.0: A comprehensive resource for 'Omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—D1041. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.
^ Wishart, David S.; Knox, Craig; Guo, An Chi; Cheng, Dean; Shrivastava, Savita; Tzur, Dan; Gautam, Bijaya; Hassanali, Murtaza (2008). . „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—D906. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.
^ Ghose, Arup K.; Viswanadhan, Vellarkad N.; Wendoloski, John J. (1998). . „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragmental Methods: An Analysis of ALOGP and CLOGP Methods”. The Journal of Physical Chemistry A. 102 (21): 3762—3772. Bibcode:1998JPCA..102.3762G. doi:10.1021/jp980230o.
^ Tetko, Igor V.; Tanchuk, Vsevolod Yu.; Kasheva, Tamara N.; Villa, Alessandro E. P. (2001). . „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
^ Ertl, Peter; Rohde, Bernhard; Selzer, Paul (2000). . „Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

Literatura

Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.

Spoljašnje veze

Tacrolimus

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] Kino T, Hatanaka H, Hashimoto M, Nishiyama M, Goto T, Okuhara M, Kohsaka M, Aoki H, Imanaka H: FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics. J Antibiot (Tokyo). . . 40 (9): 1249—55. 1987 Sep. PMID 2445721. Проверите вредност парамет(а)ра за датум: |date= (помоћ); Недостаје или је празан параметар |title= (помоћ)

[2] Pritchard DI. . „Sourcing a chemical succession for cyclosporin from parasites and human pathogens”. Drug Discov Today. 10 (10): 688—91. 2005 May 15. PMID 15896681. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[3] Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, Schreiber SL. . „Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes”. Cell. 66 (4): 807—15. 1991 Aug 23. PMID 1715244. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[4] Fukatsu S, Fukudo M, Masuda S, Yano I, Katsura T, Ogura Y, Oike F, Takada Y, Inui K. . „Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient”. Drug Metab Pharmacokinet. 21 (2): 122—5. 2006 Apr. PMID 16702731. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[5] Hanifin JM, Paller AS, Eichenfield L, Clark RA, Korman N, Weinstein G, Caro I, Jaracz E, Rico MJ: Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis. J Am Acad Dermatol. 2005 Aug;53(2 Suppl 2):S186-94. . . PMID 16021174. Недостаје или је празан параметар |title= (помоћ)

[6] Knox, C.; Law, V.; Jewison, T.; Liu, P.; Ly, S.; Frolkis, A.; Pon, A.; Banco, K.; Mak, C.; Neveu, V.; Djoumbou, Y.; Eisner, R.; Guo, A. C.; Wishart, D. S. (2011). . „DrugBank 3.0: A comprehensive resource for 'Omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—D1041. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.

[7] Wishart, David S.; Knox, Craig; Guo, An Chi; Cheng, Dean; Shrivastava, Savita; Tzur, Dan; Gautam, Bijaya; Hassanali, Murtaza (2008). . „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—D906. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.

[8] Ghose, Arup K.; Viswanadhan, Vellarkad N.; Wendoloski, John J. (1998). . „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragmental Methods: An Analysis of ALOGP and CLOGP Methods”. The Journal of Physical Chemistry A. 102 (21): 3762—3772. Bibcode:1998JPCA..102.3762G. doi:10.1021/jp980230o.

[9] Tetko, Igor V.; Tanchuk, Vsevolod Yu.; Kasheva, Tamara N.; Villa, Alessandro E. P. (2001). . „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.

[10] Ertl, Peter; Rohde, Bernhard; Selzer, Paul (2000). . „Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

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