Tolazolin

Tolazolin
(IUPAC) ime
2-benzil-4,5-dihidro-1H-imidazol
Klinički podaci
AHFS/Drugs.com Internacionalno ime leka
Identifikatori
CAS broj 59-98-3
ATC kod C04AB02 M02AX02 QV03AB94
PubChem[1][2] 5504
DrugBank DB00797
ChemSpider[3] 5303
UNII CHH9H12AQ3 DaY
KEGG[4] D08614 DaY
ChEBI CHEBI:28502 DaY
ChEMBL[5] CHEMBL770 DaY
Hemijski podaci
Formula C10H12N2 
Mol. masa 160,216 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene IV

Tolazolin je neselektivni kompetitivni antagonist α-adrenergičkog receptora. On je vazodilatator koji se koristi za tretiranje spazama perifernih krvnih sudova (kao u akrocijanozi). On je takođe uspešno korišćen kao antidot za poništavanje jake periferne vazokonstrikcije koja se može javiti usled predoziranja pojedinih agonista 5-HT2A receptora kao što su LSD, DOB i Bromo-DragonFLY, koji mogu da dovedu do gangrene ako se ne tretiraju.[6][7]

On se najčešće koristi u veterini, za poništavanje ksilazinom indukovane sedacije.[8][9]

Hemija

[uredi | uredi kod]

Tolazolin, 2-benzil-2-imidazolin, se može sintetisati putem heterociklizacije ethil ester iminofenzilsirćetne kiseline sa etilen diaminom. Struktura tolazolina je veoma slična sa α-adrenergičkim agonistima, koji su antiedemski simpatomimetici.[10][11][12][13]

Reference

[uredi | uredi kod]
  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. ↑ Bowen JS, Davis GB, Kearney TE, Bardin J. Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion. Journal of the American Medical Association 1983 Mar 18;249(11):1477-9. PMID 6827726
  7. ↑ Thorlacius K, Borna C, Personne M. Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case. (Swedish) Lakartidningen. 2008 Apr 16-22;105(16):1199-200. PMID 18522262
  8. ↑ Boothe DM (2001). „Anticonvulsant drugs and analeptic agents”. u: Adams HR (ed.). Veterinary pharmacology and therapeutics. Ames: Iowa State University Press. str. 378–9. ISBN 0-8138-1743-9.  Retrieved September 8, 2008.
  9. ↑ Hall LW, Clarke KW, Trim CM (2001). „Principles of sedation, analgesia and premedication”. Veterinary anaesthesia. Philadelphia: W.B. Saunders. str. 90–1. ISBN 0-7020-2035-4. 
  10. ↑ A. Sonn, U.S. Patent 2.161.938 (1939).
  11. ↑ W. Wustrow, P. Herold, DE 615527  (1934).
  12. ↑ M. Hartmann, H.O. Isler, DE 687196  (1938).
  13. ↑ N. Guenter, DE 3043562  (1982).

Literatura

[uredi | uredi kod]
  • Boothe DM (2001). „Anticonvulsant drugs and analeptic agents”. u: Adams HR (ed.). Veterinary pharmacology and therapeutics. Ames: Iowa State University Press. str. 378–9. ISBN 0-8138-1743-9.  Retrieved September 8, 2008 .
  • Hall LW, Clarke KW, Trim CM (2001). „Principles of sedation, analgesia and premedication”. Veterinary anaesthesia. Philadelphia: W.B. Saunders. str. 90–1. ISBN 0-7020-2035-4. 

Spoljašnje veze

[uredi | uredi kod]
Portal Medicina
Portal Hemija