Amoksapin Садржај
Farmakologija
Reference
Vidi još
Spoljašnje veze
Мени за навигацијуMonografijaa68220214028-44-5WHO2170201DB005432085R63VQ857OTD00228CHEBI:2675CHEMBL11136764165„Pharmacological profile of antidepressants and related compounds at human monoamine transporters”953782110.1016/S0014-2999(97)01393-9„Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor”887602310.1007/BF02246453„Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors”15721011082180010.1038/sj.bjp.07033411666997„Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors”7908055„Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro”6086881„Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist”1613569910.1124/jpet.105.0921551966571„Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist”1594703610.1124/jpet.105.087965уууууу
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Amoksapin (Amokisan, Asendin, Asendis, Defanil, Demoloks, Moksadil) je tetraciklični antidepresiv iz dibenzoksazepinske familije, mada se on često klasifikuje kao sekundarni aminski triciklični antidepresiv. On je N-demetilisani metabolit Loksapina.
Садржај
1Farmakologija
2Reference
3Vidi još
4Spoljašnje veze
Farmakologija
Amoksapin ispoljava mnoštvo farmakoloških efekata. On je umeren i jak inhibitor preuzimanja serotonina i norepinefrina, respektivno,[2] i vezuje se za 5-HT2A,[3]5-HT2B,[4]5-HT2C,[3]5-HT3,[5]5-HT6,[6]5-HT7,[6]D2,[7]α1-adrenergički,[7]D3[8], D4,[8] i H1 receptor[7] sa promenljivim ali značajnim afinitetom, na njijima deluje kao antagonist (ili inverzni agonist u zavisnosti od receptora) na svim aktivnim mestima. On ima slab i zanemarljiv afinitet za dopaminski transporter i 5-HT1A,[5]5-HT1B,[5]D1,[9]α2-adrenergički,[7]H4,[10]mACh,[7] i GABAA receptor,[9] i nema afiniteta za β-adrenergičke receptore ili za alosterna benzodiazepinska mesta na GABAA receptoru.[9]
^Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). „Pharmacological profile of antidepressants and related compounds at human monoamine transporters”. European Journal of Pharmacology. 340 (2–3): 249—58. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9.
↑ 3,03,1Pälvimäki EP; Roth BL; Majasuo H; et al. (1996). „Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor”. Psychopharmacology. 126 (3): 234—40. PMID 8876023. doi:10.1007/BF02246453.CS1 одржавање: Експлицитна употреба et al. (веза)
^Glusa E, Pertz HH (2000). „Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors”. British Journal of Pharmacology. 130 (3): 692—8. PMC 1572101 . PMID 10821800. doi:10.1038/sj.bjp.0703341.
↑ 5,05,15,2Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M (1991). „[Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]”. L'Encéphale (на језику: French). 17 Spec No 3: 415—22. PMID 1666997.CS1 одржавање: Непрепознат језик (веза)
↑ 6,06,1Roth BL; Craigo SC; Choudhary MS; et al. (1994). „Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors”. The Journal of Pharmacology and Experimental Therapeutics. 268 (3): 1403—10. PMID 7908055.CS1 одржавање: Експлицитна употреба et al. (веза)
↑ 7,07,17,27,37,4Richelson E, Nelson A (1984). „Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro”. The Journal of Pharmacology and Experimental Therapeutics. 230 (1): 94—102. PMID 6086881.
↑ 8,08,1Burstein ES; Ma J; Wong S; et al. (2005). „Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist”. The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1278—87. PMID 16135699. doi:10.1124/jpet.105.092155.CS1 одржавање: Експлицитна употреба et al. (веза)
↑ 9,09,19,2Wei HB, Niu XY (1990). „[Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]”. Yao Xue Xue Bao = Acta Pharmaceutica Sinica (на језику: Chinese). 25 (12): 881—5. PMID 1966571.CS1 одржавање: Непрепознат језик (веза)
^Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (2005). „Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist”. The Journal of Pharmacology and Experimental Therapeutics. 314 (3): 1310—21. PMID 15947036. doi:10.1124/jpet.105.087965.
Vidi još
Loksapin
Spoljašnje veze
Портал Medicina
Портал Hemija
п
р
у
Antidepresivi (N06A)
Specifični inhibitori preuzimanja (RI), pojačavači (RE), i agensi oslobađanja (RA)
#WHO-EM ·‡Povučeni sa tržišta · Klinička ispitivanja: †Faza III ·§Nije dospeo do faze III
M: PSO/PSI
mepr
dsrd (o,d,b,p,a,s), spec, spvo
proc, lek(N5A/5B/5C/6A/6B/6D)
п
р
у
Adrenergici
Ligandi receptora
α1
Agonisti: 5-FNE
6-FNE
Amidefrin
Anisodamin
Anisodin
Cirazolin
Dipivefrin
Dopamin
Efedrin
Epinefrin (Adrenalin)
Etilefrin
Etilnorepinefrin
Indanidin
Levonordefrin
Metaraminol
Metoksamin
Metildopa
Midodrin
Nafazolin
Norepinefrin (Noradrenalin)
Oktopamin
Oksimetazolin
Fenilefrin
Fenilpropanolamin
Pseudoefedrin
Sinefrin
Tetrahidrozolin
Antagonisti: Abanohil
Adimolol
Ajmalicin
Alfuzosin
Amosulalol
Arotinolol
Atiprosin
Benoksatian
Buflomedil
Bunazosin
Karvedilol
CI-926
Korinantin
Dapiprazol
DL-017
Domesticin
Doksazosin
Eugenodilol
Fenspirid
GYKI-12,743
GYKI-16,084
Indoramin
Ketanserin
L-765,314
Labetalol
Mefendioksan
Metazosin
Monatepil
Moksisilit (Timoksamin)
Naftopidil
Nantenin
Neldazosin
Nicergolin
Niguldipin
Pelanserin
Fendioksan
Fenoksibenzamin
Fentolamin
Piperoksan
Prazosin
Hinazosin
Ritanserin* RS-97,078
SGB-1,534
Silodosin
SL-89.0591
Spiperon
Talipeksol
Tamsulosin
Terazosin* Tibalosin
Tiodazosin
Tipentosin
Tolazolin
Trimazosin
Upidosin
Urapidil
Zolertin
* Mnogi TCA, TeCA, antipsihotici, ergolini, i neki piperazini kao što su buspiron, trazodon, nefazodon, etoperidon, i mepiprazol takođe antagoniziraju α1-adrenergičke receptore, što doprinosi njihovim nuspojavama.
α2
Agonisti: (R)-3-Nitrobifenilin
4-NEMD
6-FNE
Amitraz
Apraklonidin
Brimonidin
Kanabivarin
Klonidin
Detomidin
Deksmedetomidin
Dihodroergotamin
Dipivefrin
Dopamin
Efedrin
Ergotamin
Epinefrin (Adrenalin)
Esprohin
Etilefrin
Etilnorepinefrin
Gvanabenz
Gvanfacin
Gvanoksabenz
Levonordefrin
Lofeksidin
Medetomidin
Metildopa
Mivazerol
Nafazolin
Norepinefrin (Noradrenalin)
Fenilpropanolamin
Piperoksan
Pseudoefedrin
Rilmenidin
Romifidin
Talipeksol
Tetrahidrozolin
Tizanidin
Tolonidin
Urapidil
Ksilazin
Ksilometazolin
Antagonisti: 1-PP
Adimolol
Aptazapin
Atipamezol
BRL-44408
Buflomedil
Cirazolin
Efaroksan
Esmirtazapin
Fenmetozol
Fluparoksan
GYKI-12,743
GYKI-16,084
Idazoksan
Mianserin
Mirtazapin
MK-912
NAN-190
Olanzapin
Fentolamin
Fenoksibenzamin
Piperoksan
Piribedil
Rauvolscin
Rotigotin
SB-269,970
Setiptilin
Spiroksatrin
Sunepitron
Tolazolin
Johimbin
* Mnogi atipični antipsihotici i azapironi poput buspirona i gepirona (putem metabolita 1-PP) takođe antagonizuju α2-adrenergičke receptore.
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