Klonidin

Klonidin
(IUPAC) ime
	N-(2,6-dihlorofenil)-4,5-dihidro-1H-imidazol-2-amin
Klinički podaci
Robne marke	Catapres
AHFS/Drugs.com	Monografija
MedlinePlus	a682243
Identifikatori
CAS broj	4205-90-7
ATC kod	C02AC01 N02CX02, S01EA04
PubChem	2803
DrugBank	DB00575
ChemSpider	2701
UNII	MN3L5RMN02
KEGG	D00281
ChEBI	CHEBI:3757
ChEMBL	CHEMBL134
Hemijski podaci
Formula	C9H9Cl2N3
Mol. masa	230,093 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14) ; Key: GJSURZIOUXUGAL-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	75-95%
Vezivanje za proteine plazme	20-40%
Metabolizam	Hepatički do inaktivnih metabolita
Poluvreme eliminacije	12-33 sati
Izlučivanje	urin (40-50%)
Farmakoinformacioni podaci
Trudnoća	C(US)
Pravni status	℞ Prescription only
Način primene	oralno, transdermalno

Klonidin je simpatolitički lek koji se koristi za tretiranje visokog krvnog pritiska, nekih oblika bola, ADHD i anksioznog/paničnog poremećaja. On je klasifikovan kao centralno delujući α₂ adrenergički agonist.^[6]^[7]

Sinteza

Klonidin, 2-(2,6-dihlorofenilamin)imidazolin, se može sintetisati iz 2,6-dihloroanilina, reakcijom u kojom sa amonijum tiocijanatom daje N-(2,6- dihlorofenil)tioureju. Metilacija ovog produkta, i naknadna reakcija sa etilen diaminom daje klonidin.^[8]^[9]^[10]^[11]^[12]^[13]^[14]

Reference

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ 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
↑ Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
↑ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.
↑ K. Zeile, H. Staehle, K. H. Hauotman, DE 1303141 (1961).
↑ H. Stahle, K. Zeile, U.S. Patent 3.202.660 (1965).
↑ K. Zeile, K. H. Hauotman, H. Stahle, U.S. Patent 3.236.857 (1966).
↑ Boehringer Sohn Ingelheim, BE 653933 (1964).
↑ Boehringer Sohn Ingelheim, GB 1016514 (1962).
↑ Boehringer Ingelheim GmbH, GB 1034938 (1964).
↑ US patent 3937717, Šablon:Cite patent/authors, "2-Phenylamino-imidazolines-(2)", issued 10. 2. 1976., assigned to Boehringer Ingelheim GmbH

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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

[Goodman_Gilman-6] Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.

[PDR-7] Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.

[8] K. Zeile, H. Staehle, K. H. Hauotman, DE 1303141 (1961).

[9] H. Stahle, K. Zeile, U.S. Patent 3.202.660 (1965).

[10] K. Zeile, K. H. Hauotman, H. Stahle, U.S. Patent 3.236.857 (1966).

[11] Boehringer Sohn Ingelheim, BE 653933 (1964).

[12] Boehringer Sohn Ingelheim, GB 1016514 (1962).

[13] Boehringer Ingelheim GmbH, GB 1034938 (1964).

[14] US patent 3937717, Šablon:Cite patent/authors, "2-Phenylamino-imidazolines-(2)", issued 10. 2. 1976., assigned to Boehringer Ingelheim GmbH

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