Maprotilin

Maprotilin
(IUPAC) ime
	N-Metil- 9,10-etanoantracen- 9(10H)- propanamin
Klinički podaci
AHFS/Drugs.com	Monografija
MedlinePlus	a682158
Identifikatori
CAS broj	10262-69-8
ATC kod	N06AA21
PubChem	4011
DrugBank	DB00934
ChemSpider	3871
UNII	2U1W68TROF
KEGG	D02566
ChEMBL	CHEMBL21731
Hemijski podaci
Formula	C20H23N
Mol. masa	277,403 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C20H23N/c1-21-14-6-12-20-13-11-15(16-7-2-4-9-18(16)20)17-8-3-5-10-19(17)20/h2-5,7-10,15,21H,6,11-14H2,1H3 ; Key: QSLMDECMDJKHMQ-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	66 do 70%
Vezivanje za proteine plazme	88%
Metabolizam	hepatički
Poluvreme eliminacije	27-58 sata
Izlučivanje	bilijarno (30%) i urin (57%) kao glukonuridi, 3 do 4% kao nepromenjen lek
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Rx-only (nije kontrolisana supstanca)
Način primene	oralno, intramuskularno, intravenozno

Maprotilin (Deprilept, Ludiomil, Psymion) je tetraciklični antidepresiv (TeCA).^[6]^[7] Četvrti prsten maprotilina se razlikuje od većine drugih tetraciklina jer je formiran kao most preko centralnog tricikličnog prstena. Maprotilin je jak inhibitor preuzimanja norepinefrina sa slabim efektima na serotoninsko i dopaminsko preuzimanje.

Maprotilin ispoljava blokirajuće dejstvo na sledećim postsinaptičkim receptorima:

Jak: H₁
Umeren: 5-HT₂, alfa₁
Slab: D₂, mACh

Farmakološki profil maprotilina objašnajva njegove antidepresivne, sedativne, anksiolitske, u simpatomimetičke aktivnosti. On takođe pokazuje jak antagonizam protiv Reserpinom indukovanih efekata u životinjskim studijama, kao i drugi klasični antidepresivi. Mada se maprotilin uglavnom ponaša kao antidepresiv prve generacije on se obično smatra antiderpesivom druge generacije.

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.

Literatura

B. Bandelow, S. Bleich, S. Kropp : Handbuch Psychopharmaka (German), 2nd. edition, 2004
Benkert, Hippius : Kompendium der Psychiatrischen Pharmakotherapie (German), 4th. edition, 2003

}{refend}}

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Maprotiline drug information Arhivirano 2001-08-10 na Wayback Machine-u
rxlist.com^{[mrtav link]}
Schweizer Arzneikompendium (German)^{[mrtav link]}
List of suppliers

[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.

[1]

[2]

[3]

[4]

[5]

[6]

[7]