| 词条 | Fludiazepam |
| 释义 |
| Watchedfields = changed | verifiedrevid = 443821344 | IUPAC_name = 7-chloro-5-(2-fluorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one | image = Fludiazepam.svg | width = 170 | image2 = Fludiazepam ball-and-stick model.png | tradename = Erispan (JP, TW) | Drugs.com = {{drugs.com|international|fludiazepam}} | pregnancy_category = | legal_CA = Schedule IV | legal_DE = Anlage III | legal_US = Schedule IV | routes_of_administration = Oral (tablets) | bioavailability = | metabolism = Hepatic | elimination_half-life = | excretion = Renal | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 3900-31-0 | ATC_prefix = N05 | ATC_suffix = BA17 | PubChem = 3369 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB01567 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3252 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 7F64A2K16Z | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D01354 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 31618 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 13291 | C=16 | H=12 | Cl=1 | F=1 | N=2 | O=1 | molecular_weight = 302.7 | smiles = O=C1CN=C(C2=CC=CC=C2F)C3=CC(Cl)=CC=C3N1C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C16H12ClFN2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = ROYOYTLGDLIGBX-UHFFFAOYSA-N }}Fludiazepam[1], marketed under the brand name Erispan (エリスパン)[2][3] is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[4] originally developed by Hoffman-La Roche in the 1960s.[5] It is marketed in Japan and Taiwan. {{cn|date=March 2016}} It exerts its pharmacological properties via enhancement of GABAergic inhibition.[6] Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam.[7] It possesses anxiolytic,[8][9][10] anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.[11] As with all benzodiazepines, fludiazepam is used recreationally.[12] See also
References1. ^ US Patent 3371085 5-aryl-3h-1,4-benzodiazepin-2(1h)-ones 2. ^{{Cite journal | last1 = Su | first1 = TP. | last2 = Chen | first2 = TJ. | last3 = Hwang | first3 = SJ. | last4 = Chou | first4 = LF. | last5 = Fan | first5 = AP. | last6 = Chen | first6 = YC. | title = Utilization of psychotropic drugs in Taiwan: an overview of outpatient sector in 2000. | journal = Zhonghua Yi Xue Za Zhi (Taipei) | volume = 65 | issue = 8 | pages = 378–91 |date=Aug 2002 | PMID = 12455808 }} 3. ^{{cite web|url=http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html |title=Benzodiazepine Names |accessdate=2008-12-29 |publisher=non-benzodiazepines.org.uk |deadurl=yes |archiveurl=https://web.archive.org/web/20081208054743/http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html |archivedate=2008-12-08 |df= }} 4. ^{{Cite journal | last1 = Neville | first1 = GA. | last2 = Beckstead | first2 = HD. | last3 = Shurvell | first3 = HF. | title = A Fourier transform-Raman and infrared vibrational study of delorazepam, fludiazepam, flurazepam, and tetrazepam. | journal = J Pharm Sci | volume = 83 | issue = 2 | pages = 143–51 |date=Feb 1994 | PMID = 7909552 | doi=10.1002/jps.2600830207}} 5. ^US Patent 3299053 -ARYL-JH-L,X-BENZODIAZEPIN-Z(LH)-ONES 6. ^{{Cite journal | last1 = Tsuchiya | first1 = T. | last2 = Fukushima | first2 = H. | title = Effects of benzodiazepines and pentobarbitone on the gaba-ergic recurrent inhibition of hippocampal neurons. | journal = Eur J Pharmacol | volume = 48 | issue = 4 | pages = 421–4 |date=Apr 1978 | PMID = 648585 | doi=10.1016/0014-2999(78)90169-3}} 7. ^{{Cite journal | last1 = Nakatsuka | first1 = I. | last2 = Shimizu | first2 = H. | last3 = Asami | first3 = Y. | last4 = Katoh | first4 = T. | last5 = Hirose | first5 = A. | last6 = Yoshitake | first6 = A. | title = Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. | journal = Life Sci | volume = 36 | issue = 2 | pages = 113–9 |date=Jan 1985 | pmid = 2857046 | doi=10.1016/0024-3205(85)90089-X}} 8. ^{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Effect of an anxiolytic on lipid profile in non-insulin-dependent diabetes mellitus. | journal = J Int Med Res | volume = 22 | issue = 6 | pages = 338–42 | PMID = 7895897 | year=1994}} 9. ^{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = Improvement of stress reduces glycosylated haemoglobin levels in patients with type 2 diabetes. | journal = J Int Med Res | volume = 23 | issue = 2 | pages = 119–22 | PMID = 7601294 | year=1995}} 10. ^{{Cite journal | last1 = Okada | first1 = S. | last2 = Ichiki | first2 = K. | last3 = Tanokuchi | first3 = S. | last4 = Ishii | first4 = K. | last5 = Hamada | first5 = H. | last6 = Ota | first6 = Z. | title = How blood pressure in patients with non-insulin-dependent diabetes mellitus is influenced by stress. | journal = J Int Med Res | volume = 23 | issue = 5 | pages = 377–80 | PMID = 8529781 | year=1995}} 11. ^{{Cite journal | last1 = Inoue | first1 = H. | last2 = Maeno | first2 = Y. | last3 = Iwasa | first3 = M. | last4 = Matoba | first4 = R. | last5 = Nagao | first5 = M. | title = Screening and determination of benzodiazepines in whole blood using solid-phase extraction and gas chromatography/mass spectrometry. | journal = Forensic Sci Int | volume = 113 | issue = 1-3 | pages = 367–73 |date=Sep 2000 | pmid = 10978650 | doi=10.1016/S0379-0738(00)00226-7}} 12. ^{{Cite journal | last1 = Shimamine | first1 = M. | last2 = Masunari | first2 = T. | last3 = Nakahara | first3 = Y. | title = [Studies on identification of drugs of abuse by diode array detection. I. Screening-test and identification of benzodiazepines by HPLC-DAD with ICOS software system] | journal = Eisei Shikenjo Hokoku | issue = 111 | pages = 47–56 | year = 1993 | PMID = 7920567 }} External links
9 : Benzodiazepines|Sedatives|Hypnotics|Anticonvulsants|Anxiolytics|Lactams|Chloroarenes|Fluoroarenes|GABAA receptor positive allosteric modulators |
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