Ciproheptadin
IUPAC ime | |
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4-(5H-dibenzo [a,d]ciklohepten-5-iliden)-1-metilpiperidin hidrohlorid | |
Klinički podaci | |
Prodajno ime | Periaktin |
Drugs.com | Monografija |
MedlinePlus | a682541 |
Kategorija trudnoće |
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Način primene | Oralno |
Pravni status | |
Pravni status |
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Farmakokinetički podaci | |
Vezivanje proteina | 96 do 99% |
Metabolizam | Hepatički i renalno |
Poluvreme eliminacije | 8,6 sata[1] |
Izlučivanje | Fekalno i renalno |
Identifikatori | |
CAS broj | 129-03-3 Y 969-33-5 (hidrohlorid) |
ATC kod | R06AX02 (WHO) |
PubChem | CID 2913 |
IUPHAR/BPS | 277 |
DrugBank | DB00434 Y |
ChemSpider | 2810 Y |
UNII | 2YHB6175DO Y |
KEGG | D07765 Y |
ChEBI | CHEBI:4046 Y |
ChEMBL | CHEMBL516 Y |
Hemijski podaci | |
Formula | C21H21N |
Molarna masa | 287,398 g/mol |
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Ciproheptadin (Periaktin) je prva generacija antihistamina sa dodatnim antiholinergičnim, antiserotinergičnim, i lokalno anestetičkim svojstvima.[2][3]
Farmakologija
Ciproheptadin deluje kao antagonist (ili inverzni agonist u zavisnosti od aktivnog mesta) na sledećim receptorima:
- H1 (~0,05 nM)[4] > 5-HT2A (~2 nM)[5] ≈ 5-HT2B (~1,5 nM)[6] ≈ 5-HT2C (~2 nM)[6] > mACh (M1-M5; ~7-12 nM)[7] ≈ D3 (~8 nM)[8]
On ima slab, i verovatno zanemarljiv, afinitet za sledeća mesta vezivanja (Ki):
- 5-HT1A (~60-100 nM)[5][8] ≈ α1-adrenergički (?? nM)[9] ≈ α2-adrenergički (?? nM)[9] > 5-HT6 (~135-150 nM)[10][11] ≈ 5-HT7 (~125 nM)[11] ≈ D1 (~115 nM)[8] ≈ D2 (~115 nM)[8] > 5-HT3</sub> (~250 nM)[8][12] ≈ NET (~300 nM)[13]
Pored toga, ciproheptadin poseduje osobine blokatora kalcijumskog kanala[14] i lokalnog anestetika.[15]
Reference
- ^ Gunja N, Collins M, Graudins A (2004). „A comparison of the pharmacokinetics of oral and sublingual cyproheptadine”. Journal of Toxicology. Clinical Toxicology. 42 (1): 79—83. PMID 15083941.
- ^ 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.
- ^ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.
- ^ Moguilevsky, N.; F, Varsalona; Noyer, M.; et al. (1994). „Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene”. European Journal of Biochemistry / FEBS. 224 (2): 489—95. PMID 7925364. doi:10.1111/j.1432-1033.1994.00489.x.
- ^ а б Peroutka, S. J. (1988). „Antimigraine drug interactions with serotonin receptor subtypes in human brain”. Annals of Neurology. 23 (5): 500—4. PMID 2898916. doi:10.1002/ana.410230512.
- ^ а б Bonhaus, D. W.; Weinhardt, K. K.; Taylor, M.; et al. (1997). „RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist”. Neuropharmacology. 36 (4–5): 621—9. PMID 9225287. doi:10.1016/S0028-3908(97)00049-X.
- ^ Stanton T, Bolden-Watson C, Cusack B, Richelson E (1993). „Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics”. Biochemical Pharmacology. 45 (11): 2352—4. PMID 8100134. doi:10.1016/0006-2952(93)90211-E.
- ^ а б в г д Toll, L.; Berzetei-Gurske IP; Polgar, W. E.; et al. (1998). „Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications”. NIDA Research Monograph. 178: 440—66. PMID 9686407.
- ^ а б Dukhovich, F. S. (15. 8. 2005). Pharmacological aspects of molecular recognition. Nova Publishers. стр. 117. ISBN 978-1-59454-676-1. Приступљено 27. 11. 2011.
- ^ Kohen, R.; Metcalf, M. A.; Khan, N.; et al. (1996). „Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor”. Journal of Neurochemistry. 66 (1): 47—56. PMID 8522988. doi:10.1046/j.1471-4159.1996.66010047.x.
- ^ а б Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL (1993). „Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase”. The Journal of Biological Chemistry. 268 (31): 23422—6. PMID 8226867.
- ^ Hoyer D, Neijt HC (1988). „Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding”. Molecular Pharmacology. 33 (3): 303—9. PMID 3352595.
- ^ Runyon SP, Savage JE, Taroua M, Roth BL, Glennon RA, Westkaemper RB (2001). „Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene”. Bioorganic & Medicinal Chemistry Letters. 11 (5): 655—8. PMID 11266163. doi:10.1016/S0960-894X(01)00023-3.
- ^ Lowe DA, Matthews EK, Richardson BP (1981). „The calcium antagonistic effects of cyproheptadine on contraction, membrane electrical events and calcium influx in the guinea-pig taenia coli”. British Journal of Pharmacology. 74 (3): 651—63. PMC 2071752 . PMID 6271323.
- ^ F, Riccioppo Neto (1979). „The local anesthetic effect of cyproheptadine on mammalian nerve fibres”. European Journal of Pharmacology. 54 (3): 203—7. PMID 428422. doi:10.1016/0014-2999(79)90078-5.
Literatura
- Dukhovich, F. S. (2005). Pharmacological aspects of molecular recognition. Nova Publishers. стр. 117. ISBN 978-1-59454-676-1. Приступљено 27. 11. 2011.
Spoljašnje veze
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