药物代谢研究工具药

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1、? 88 ? ? A ? 31 ? 3109 ? http:Tel: 025-83204231/84715147Fax: 025-83204231 Email:http:/http:/http:/http:/? ? ?Nanjing DeBioChem Reagent $?=-?=-=-A=-?=?BCDE?-? ?FG0?H?I*6? !“#JK$LMN?OP40QR4?ST? UVMN6GRW?4MXYZ Chiral Chiral Chiral Chiral Reagent Reagent Reagent Reagent ? ? !“#? ?$% ?+?CAS A?B?CD?EFGHI

2、JKL? Enzyme Inhibitors/Substrates/ActivatorsEnzyme Inhibitors/Substrates/ActivatorsEnzyme Inhibitors/Substrates/ActivatorsEnzyme Inhibitors/Substrates/Activators ?Histone Deacetylase MNOPQRST;Aldose Reductase UVWXT;ATPase Modulators YZT;Cyclooxygenase _T;Lipoxygenase _ T;GTPase aYZT;HMG-CoA Reductas

3、e -b- -cSdefRgT A W XT;Monoamine Oxidase fh_+T;Protease NOT Enzyme Substrates / Activators i? 789:;? Reagents for Drug metabolism Research Reagents for Drug metabolism Research Reagents for Drug metabolism Research Reagents for Drug metabolism Research ?q*?rs3tu3vw?$%xy.z?|? !)? ?K?vw?.? ? 789:;9?)?

4、ABCD p450 EFGHI2d?Ke?!“fg?hi.j?klm?noc?pqr?k!?.Ks?d?e?!?.j?k_?.Ks?b?T?F?W)?.c?)?n?:/.?“b6x?.?+fi?U?fl?Yofifl?X”bABCD P450 ?PyI2FV?.? 450nm ?P450 ?sZ?ABCD?ab?ABCD P450 ?:;?.n?;V?G?Z?e?W !?ZY?“?#$%? !?JK?L?“W?yj“?ABCD P450S?EM?481zP450#3V22zN#3 ?OPQ 1995 ? 10 R! ST? 74 z#3N.?Z?UM? 14 z#3N.?Ur?Z?#3? 20

5、 zMN? ? ? ?VzABCD P450 ?)?3?.?o.“uv:?2F?o CYP1A d#?ABCD P450 ?XY?,-?E.CYP3A QR?, P450 ? 30%.CYP2 QR 20%.CYP1A2 R 13%. CYP2E1 R 7%. CYP2A6 R 4%.CYP2D6 R 2%?B?.?BAB?r?d?,ABCD P450?z?.ABCD P450 ? CYP3A4 ?6?. CYP1A1?6?e?e?CYP2D6 ? CYP2C8-10 ?Vfl?flurasepam!=?ABCD P450 Xe? ?mV_?.?r?yKsqi?P YP2D6 ?flCYP2C

6、19?w+6,3.?(t.m?z?/?pB?oH+?V?0ab.o13?23?3s.CYP2D6?223kH/?.?.?Z?,?/0E?E?jmyt?A?-?B?s#*?CD?“?E!oas CYP2D6 :?A? XA? CYP1A2 ?F73.CYP3A4 ?G:H3?E?_b?/0.()3sIJ.?K?LM?b:NX CYP3A ?t?V?D?D?ouv CYP3A uv CYP2E1 ?ab?(?3?o?Fb?.;?.nX?H?kuv CYP2E1 OP?r?flfl ?fifl fl ?VIfls!?ABCD P450 X P450 w+6?V NADPH ?CYP2E1? 2A6

7、? 3A ?6?IflsVfiflfl?yfl=Ifls4fl?i?fi flflq3?10 ?.-?Afl?.?hfl2?V?.ABCD?X?h?oH?+?ABCD P450?2?h?9?ab?CYP1A2V3A4? 88 ? ? A ? 31 ? 3109 ? http:Tel: 025-83204231/84715147Fax: 025-83204231 Email:N-methyl-3-(2-methylphenoxy)-3-phenyl-propan-1-a mine 82248-59 -7 C17H21NO255.4 solid;Store at RTAntidepressant

8、Atomoxetine is an amphetamine used to treat ADD/ADHD in children and adults. Attention-Deficit/Hyperactivity Disorder. CYP 2D6PP-C010Atorvastatin *?7-2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)- 5-propan-2-yl-pyrrol-1-y l-3,5- dihydroxy-heptanoic acid 134523-00-5; C33H35FN2O5558.6 solid;Store at

9、 RTAnticholesteremic Agent; HMG-CoA Reductase It inhibitors selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. CYP3A4.5

10、.7 PP-C011Bufuralol AB()59652-29 -8 C16H24CINO2?297.82 solid; Store at -20C Dissolve in 0.1M Potassium Phosphate Buffer at a concentration of 1 mM.Bufuralol is the substrate for the Bufuralol 1-Hydroxylase Assay in CYP2D6.1-Hydroxybufuraol is the generated metabolite in this reaction. CYP 2D6 PP-C01

11、2BupropionA#CD1-(3-chlorophenyl)-2-tert-butylamino-propan-1-one “#34841-39 -9 ; C13H18ClNO; 239.74 |o31677-93 -7 ; C13H18ClNOHCl276.2 solid;Store at RTAntidepressant Bupropion selectively inhibits the neuronal reuptake of dopamine, norepinephrine, and serotonin CYP 2B6PP-C013Buspirone AEFD8-4-(4-pyr

12、imidin-2-ylpiperazin-1-yl)butyl-8-azaspir o4.5decane-7,9-dione 36505-84 -7 ; C21H31N5O2385.5 solid;Store at RTAnti-anxiety Agent, Serotonin Agonist Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhi

13、biting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP) CYP 3A4 PP-C014 GCaffeine HIJ1,3,7-trimethyl-3,7-dihydropurine-2,6-dione 58-08-2; C8H10N4O2194.2 solid;Store at RTC

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