| 词条 | Bifemelane |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 459721492 | IUPAC_name = N-methyl-4-[2-(phenylmethyl)phenoxy]butan-1-amine | image = Bifemelane.svg | width = 235 | tradename = Alnert, Celeport | Drugs.com = {{drugs.com|international|bifemelane}} | routes_of_administration = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 90293-01-9 | ATC_prefix = N06 | ATC_suffix = AX08 | PubChem = 2377 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 1192517 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = Z4501GN13G | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 2286 | smiles = O(c1ccccc1Cc2ccccc2)CCCCNC | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C18H23NO/c1-19-13-7-8-14-20-18-12-6-5-11-17(18)15-16-9-3-2-4-10-16/h2-6,9-12,19H,7-8,13-15H2,1H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = QSQQPMHPCBLLGX-UHFFFAOYSA-N | synonyms = MCl-2016 | C=18 | H=23 | N=1 | O=1 | molecular_weight = 269.381 g/mol }}Bifemelane (INN) (Alnert, Celeport), or bifemelane hydrochloride (JAN), also known as 4-(O-benzylphenoxy)-N-methylbutylamine, is an antidepressant and cerebral activator that is widely used in the treatment of cerebral infarction patients with depressive symptoms in Japan, and in the treatment of senile dementia as well.[1][2] It also appears to be useful in the treatment of glaucoma.[3] Bifemelane acts as a monoamine oxidase inhibitor (MAOI) of both isoenzymes, with competitive (reversible) inhibition of MAO-A (Ki = 4.20 μM) (making it a reversible inhibitor of monoamine oxidase A (RIMA)) and non-competitive (irreversible) inhibition of MAO-B (Ki = 46.0 μM),[4][5][6] and also acts (weakly) as a norepinephrine reuptake inhibitor.[7] The drug has nootropic, neuroprotective, and antidepressant-like effects in animal models, and appears to enhance the cholinergic system in the brain.[8][9][10] See also
References1. ^{{cite journal | vauthors = Koide S, Onishi H, Hashimoto H, Kai T, Katayama M, Yamagami S | title = Effects of bifemelane hydrochloride on plasma neuropeptide Y, 3-methoxy-4-hydroxyphenylethylene glycol and 5-hydroxy-indole acetic acid concentrations in patients with cerebral infarction | journal = Drugs Exp Clin Res | volume = 21 | issue = 5 | pages = 175–80 | year = 1995 | pmid = 8846747 | doi = | url = }} {{Antidepressants}}{{Antidementia}}{{Nootropics}}{{Adrenergics}}{{Dopaminergics}}{{Serotonergics}}{{nervous-system-drug-stub}}2. ^{{cite book | author = David J. Triggle | title = Dictionary of Pharmacological Agents | publisher = Chapman & Hall/CRC | location = Boca Raton | year = 1996 | page = 265 | isbn = 978-0-412-46630-4 | oclc = | doi = | url = https://books.google.com/books?id=DeX7jgInYFMC&lpg=RA1-PA265&dq=bifemelane%20Alnert%20Celeport&pg=RA1-PA265#v=onepage&q=&f=false}} 3. ^{{cite journal | last1 = Shigemitsu | first1 = T | last2 = Majima | first2 = Y | title = Use of bifemelane hydrochloride in improving and maintaining the visual field of patients with glaucoma | journal = Clinical Therapeutics | volume = 18 | issue = 1 | pages = 106–13 | year = 1996 | pmid = 8851457 | doi = 10.1016/S0149-2918(96)80183-4 }} 4. ^{{cite journal|last1=Naoi|first1=Makoto|last2=Nomura|first2=Yoshio|last3=Ishiki|first3=Ryoji|last4=Suzuki|first4=Hiroko|last5=Nagatsu|first5=Toshiharu|title=4-(O-Benzylphenoxy)-N-Methylbutylamine (Bifemelane) and Other 4-(O-Benzylphenoxy)-N-Methylalkylamines as New Inhibitors of Type A and B Monoamine Oxidase|journal=Journal of Neurochemistry|volume=50|issue=1|year=1988|pages=243–247|issn=0022-3042|doi=10.1111/j.1471-4159.1988.tb13256.x}} 5. ^{{cite journal|last1=Kovel'man|first1=I. R.|last2=Tochilkin|first2=A. I.|last3=Gorkin|first3=V. Z.|title=Structure and action of reversible monoamine oxidase inhibitors (review)|journal=Pharmaceutical Chemistry Journal|volume=25|issue=8|year=1991|pages=505–520|issn=0091-150X|doi=10.1007/BF00777412}} 6. ^{{cite book|author=Jae Y. Choe|title=Drug Actions and Interactions|url=https://books.google.com/books?id=BZeTPw_GgbgC|date=4 March 2011|publisher=McGraw Hill Professional|isbn=978-0-07-176945-7|page=307}} 7. ^{{cite book|last1=Dostert|first1=P.|title=Amine Oxidases: Function and Dysfunction|chapter=Can our knowledge of monoamine oxidase (MAO) help in the design of better MAO inhibitors?|year=1994|pages=269–279|doi=10.1007/978-3-7091-9324-2_35|quote=For example, bifemelane [4-(O-benzylphenoxy)-N-methylbutylamine) is one of the few molecules in which both activities, reversible inhibition of MAO-A (Naoi et al., 1988) and inhibition of noradrenaline uptake (Egawa et al., 1983), although weak (IC50 = 10-6-10-7 M), coexist.|isbn=978-3-211-82521-1}} 8. ^{{cite journal | last1 = Kondo | first1 = Y | last2 = Ogawa | first2 = N | last3 = Asanuma | first3 = M | last4 = Matsuura | first4 = K | last5 = Nishibayashi | first5 = K | last6 = Iwata | first6 = E | title = Preventive effects of bifemelane hydrochloride on decreased levels of muscarinic acetylcholine receptor and its mRNA in a rat model of chronic cerebral hypoperfusion | journal = Neuroscience Research | volume = 24 | issue = 4 | pages = 409–14 | year = 1996 | pmid = 8861111 | doi = 10.1016/0168-0102(95)01017-3 }} 9. ^{{cite journal | last1 = Egashira | first1 = T | last2 = Takayama | first2 = F | last3 = Yamanaka | first3 = Y | title = Effects of bifemelane on muscarinic receptors and choline acetyltransferase in the brains of aged rats following chronic cerebral hypoperfusion induced by permanent occlusion of bilateral carotid arteries | journal = Japanese Journal of Pharmacology | volume = 72 | issue = 1 | pages = 57–65 | year = 1996 | pmid = 8902600 | doi = 10.1254/jjp.72.57 }} 10. ^{{cite journal |vauthors=Moryl E, Danysz W, Quack G | title = Potential antidepressive properties of amantadine, memantine and bifemelane | journal = Pharmacology & Toxicology | volume = 72 | issue = 6 | pages = 394–7 |date=June 1993 | pmid = 8361950 | doi = 10.1111/j.1600-0773.1993.tb01351.x| url = }} 7 : Amines|Antidepressants|Monoamine oxidase inhibitors|Nootropics|Norepinephrine reuptake inhibitors|Phenol ethers|Reversible inhibitors of MAO-A |
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