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1 as the site of covalent modification by the active metabolite.
2 enhance the conversion of clopidogrel to its active metabolite.
3 ation of flutamide and hydroxyflutamide, its active metabolite.
4 azen-1-yl)imidazole-4-carboximide] MTIC, its active metabolite.
5 ndex, and PK by plasma levels of prasugrel's active metabolite.
6 cleavage for the release of the biologically active metabolite.
7 d in biotransformation of clopidogrel to its active metabolite.
8 ene (CYP2D6), oxidizes tamoxifen to its most active metabolites.
9 te a response to endogenously produced redox-active metabolites.
10 thotrexate, and pemetrexed to produce highly active metabolites.
11 production of toxins and other biologically active metabolites.
12 alysis to determine the presence of possible active metabolites.
13 ct possible parent compounds that might have active metabolites.
14 ting that this could be attributed to highly active metabolites.
15 er to deplete bioactive retinoids or to form active metabolites.
16 oxide metabolites produced by FMOs are often active metabolites.
17 amount of drug available for conversion into active metabolites.
22 TP is first converted to a pharmacologically active metabolite 1-methyl-4-phenylpyridinum (MPP+).
24 hages are abundant sources of PGD(2) and its active metabolite 15-deoxy-Delta(12,14)-PGJ(2) (15-d-PGJ
25 -hydroxyestrone (2OHE1), to the biologically active metabolite, 16alpha-hydroxyestrone (16alphaOHE1),
26 2) and 4.15 hours, respectively; whereas the active metabolite 17-aminogeldanamycin had a t(1/2) of 7
27 -hydroxyvitamin D(3) (25(OH)D(3)) and/or its active metabolite, 1alpha,25-dihydroxyvitamin D(3) (1,25
28 aptohept-4-enoic acid moiety to generate the active metabolite 2, which is an extraordinarily potent
36 ioconverting cyclophosphamide (CPA) into the active metabolites 4-hydroxyCPA/aldophosphamide (AP).
40 tate (NNN-5'-OAc), a stable precursor of the active metabolite 5'-hydroxy(+/-)-N'-nitrosonornicotine
42 inhibition in yields of the physiologically active metabolite 5alpha-dihydrotestosterone (DHT) in HG
43 nts, but intracellular accumulation of their active metabolites (6-thioguanine nucleotides, 6-TGN) ca
44 drolysis of the glucuronide conjugate of the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38)
46 omide was dosed to a targeted blood level of active metabolite, A77 1726, of 50 microg/ml to 100 micr
47 drug class would enhance liver levels of the active metabolite adefovir diphosphate (ADV-DP) and/or d
51 vitamin A to enzymes for metabolism into an active metabolite, all-trans retinoic acid (atRA), where
53 ur results showed that the production of the active metabolite (AM) from 2-oxoclopidogrel by human li
54 formation of a glutathionyl conjugate of the active metabolite (AM) of clopidogrel and the covalent m
55 cement of an anti-METH scFv for METH and its active metabolite amphetamine (AMP), through the introdu
56 ed biotransformation of clopidogrel into its active metabolite and decreased efficacy of clopidogrel
58 n by comparison of its induction between the active metabolite and its parent compound (B[a]PDE versu
59 nverted in rat or mouse plasma solely to two active metabolites and had significantly enhanced oral b
61 oxifen, 4-OH tamoxifen (a major biologically active metabolite), and 17beta-estradiol in native myocy
62 CYP)1A2, which converts clopidogrel into its active metabolite, and prior studies suggest greater inh
63 tion, decreases plasma levels of clopidogrel active metabolite, and retards and diminishes its effect
64 s with long-term adjuvant therapy, examining active metabolites, and considering chemoprevention all
65 ities recently entering the marketplace have active metabolites, and many more are (or have been) in
68 hine lowers the plasma levels of clopidogrel active metabolite as well as its effects on platelets.
70 uted uracil analogue is converted to several active metabolites but the mechanism of cytotoxicity has
72 Clopidogrel requires transformation into an active metabolite by cytochrome P-450 (CYP) enzymes for
74 n attenuate metabolism of clopidogrel to its active metabolite by inhibiting various hepatic CYP450 e
75 l and prasugrel require biotransformation to active metabolites by cytochrome P450 (CYP) enzymes.
76 eudomonas aeruginosa produces colorful redox-active metabolites called phenazines, which underpin bio
78 lts show that modulating extracellular redox-active metabolites can influence the fitness of a biofil
79 Ceftaroline fosamil, the prodrug form of the active metabolite ceftaroline, is a new broad-spectrum p
83 genesis in in vitro studies and implies that active metabolites contribute to its in vivo pharmacolog
86 The area under the curve for clopidogrel active metabolite decreased significantly with esomepraz
87 ucoma drugs tested only metipranolol and its active metabolite, desacetylmetipranolol, blunted the SN
89 9 alleles have significantly lower levels of active metabolite, diminished platelet inhibition, and h
90 inistration resulted in the formation of the active metabolite, diminution of tumor vasculature, and
91 technique that can detect hundreds of redox-active metabolites down to the level of femtograms on co
92 supplementation on the formation of flavour active metabolites during wine fermentation, we evaluate
93 n situ monitoring of the production of redox-active metabolites (e.g., pyocyanin) during the course o
94 urs, and peak plasma concentrations of these active metabolites exceeded 10 micromol/L after IV EMP d
95 umor activity of ICT2588 was superior to its active metabolite, exhibiting reduced toxicity, improved
99 s have demonstrated that triphosphate is the active metabolite for both these purine nucleoside analo
100 analog inhibitors, including the clinically active metabolite formed by sofosbuvir, to elucidate key
101 mercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel
102 t even the spontaneous release of NPY (or an active metabolite) from recurrent mossy fibers is suffic
103 18 to be more efficiently converted into its active metabolite, gemcitabine triphosphate (dFdCTP), an
104 ducts proved useful in the identification of active metabolites generated by either in vitro or in vi
105 has been associated with reduced clopidogrel active metabolite generation and higher ex vivo platelet
106 f a PPI with clopidogrel reduces clopidogrel active metabolite generation and subsequent platelet inh
108 h attenuates CYP2D6 metabolism and increases active metabolite half-lives and may therefore lead to s
109 Preferential hydrolysis of ICT2588 to its active metabolite (ICT2552) was observed in tumor homoge
110 ecent findings have identified lactate as an active metabolite in cell signalling, although its effec
111 ate are made available for the generation of active metabolites in platelets when the NEFA binding ca
112 earthworms possess a class of unique surface-active metabolites in their gut, which we term 'drilodef
115 ion with dithiothreitol, confirming that the active metabolite is linked to a cysteinyl residue of CY
117 oped to release the doxorubicin-formaldehyde active metabolite, is tethered via derivatized ethylene
118 elta(9)THC) is metabolized to only one major active metabolite, it has been reported that several maj
119 report here that nitazoxanide (NTZ) and its active metabolite kill replicating and nonreplicating M.
120 (SC-51) is rapidly converted in vivo to the active metabolite L-N6-(1-iminoethyl)lysine (L-NIL).
121 ibed natural substance largazole (1) and its active metabolite largazole thiol (2) is described.
123 (TDM), which involves measurement of drug or active metabolite levels and anti-drug antibodies, is a
124 ent data have surfaced demonstrating altered active metabolite levels of clopidogrel in patients harb
128 ment (thionamides such as carbimazole or its active metabolite methimazole are the drugs of choice).
129 TGN) are currently being considered as major active metabolites, methylthioinosine nucleotides seem t
130 ), which converts 25-hydroxyvitamin D to its active metabolite, might be up regulated in human colon
132 neurons, and behavioral changes due to TLR4 active metabolite, morphine-3-glucuronide (M3G) exposure
135 omilast and roflumilast; the latter (and its active metabolite N-oxide) is more selective and potent
137 dies have reported that both nitrate and its active metabolite, nitrite, have therapeutic activity in
139 like cycloguanil, however, 1a (WR99210), the active metabolite of 1, has retained in vitro potency ag
142 lves 1-methyl-4-phenylpyridinium (MPP+), the active metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydr
143 used increased selectivity for dGTP over the active metabolite of abacavir (carbovir triphosphate).
144 stance to monodesethylamodiaquine (MDAQ; the active metabolite of AQ) than to CQ, whereas a pfcrt all
145 Benzo[a]pyrene diol epoxide (BPDE), the active metabolite of benzo[a]pyrene present in tobacco s
146 50 to benzo(a)pyrene-diol-epoxide (BPDE), an active metabolite of BP in human bronchial epithelial BE
150 reduction of 32.4% in plasma exposure to the active metabolite of clopidogrel, as compared with nonca
151 allele had significantly lower levels of the active metabolite of clopidogrel, diminished platelet in
152 Almost 30% of the variability in SN-38 (the active metabolite of CPT-11) AUC is explained by ABCC1 1
153 With the combination therapy of SN-38 (the active metabolite of CPT-11) followed by flavopiridol, t
154 man colon cancer cells Hct116 with SN-38 (an active metabolite of CPT-11) resulted in G2 cell cycle a
155 sensor, which emits light in response to the active metabolite of cytosine arabinoside (ara-C, cytara
156 l variability in blood concentrations of the active metabolite of dabigatran etexilate and influence
158 , we show that 20-hydroxyecdysone (20E), the active metabolite of ecdysone that is induced by environ
159 hosphorylase (PNP) that locally converts the active metabolite of F-araAMP to a highly diffusible sub
160 tions and in complex with norfluoxetine, the active metabolite of fluoxetine (Prozac) and a state-dep
161 ecently demonstrated that FTY-phosphate, the active metabolite of FTY720, acts as a full agonist for
164 ure to cytotoxic concentration of SN-38, the active metabolite of irinotecan (0.1 microM) alone and i
165 Their response to oxaliplatin, to SN38, the active metabolite of irinotecan (drugs active in colon c
166 a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on c
167 platin, 5-fluorouracil (5-FU), or SN-38 (the active metabolite of irinotecan) induced Notch-1 intrace
168 asma concentration (Css) of total SN-38 (the active metabolite of irinotecan) was 6.42 +/- 1.10 nmol/
169 d 7-ethyl-10-hydroxycamptothecin (SN-38; the active metabolite of irinotecan), two S-phaseselective a
170 porter that confers resistance to SN-38 (the active metabolite of irinotecan), was readily detected i
172 7-ethyl-10-hydroxycamptothecin (SN-38), the active metabolite of irinotecan, in a number of differen
173 y 7-ethyl-10-hydroxycamptothecin (SN-38), an active metabolite of irinotecan, in p53-null compared wi
174 how for the first time that SN38, the potent active metabolite of irinotecan, induces c-Jun NH(2)-ter
187 s demonstrate that both ethosuximide and the active metabolite of methsuximide, alpha-methyl-alpha-ph
188 asculature than A-61603 (2), ST-1059 (3, the active metabolite of midodrine), and phenylpropanolamine
189 lpropanolamine (PPA) (1) and ST-1059 (2, the active metabolite of midodrine), supporting the hypothes
190 ncentrations of mycophenolic acid (MPA), the active metabolite of MMF, and outcomes in 85 patients wi
193 d the effect of mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil, on erythropo
194 7,8,9,10-tetrahydro benzo[a]pyrene (BPDE, an active metabolite of PAHs) induced cytotoxicity, mutagen
195 the effects of ASA, acetaminophen (APAF, the active metabolite of phenacetin), caffeine, and other re
198 4 inhibitor roflumilast N-oxide (RNO) is the active metabolite of roflumilast approved as a treatment
200 optimization, to improve the binding of the active metabolite of the anti-inflammatory drug leflunom
201 cy are comparable or superior to MRE269 (the active metabolite of the clinical compound NS-304) with
202 possible to demonstrate that vedelianin, an active metabolite of the family of prenylated stilbenes
205 ound to gemcitabine diphosphate (GemdP), the active metabolite of the mechanism-based chemotherapeuti
206 1-Methyl-4-phenylpyridinium (MPP(+)), the active metabolite of the neurotoxin 1-methyl-4-phenyl-1,
207 oxide homeostasis and suggest that it is an active metabolite of the organic nitrates that can be us
208 in-2-yl)phenyl)-3-(pyridin-4-yl)urea (2), an active metabolite of the potent PI3 kinase inhibitor PKI
211 1 (1 microM) prior to exposure to SN-38, the active metabolite of the topoisomerase I inhibitor, CPT-
212 roteins for all-trans-retinoic acid (RA), an active metabolite of vitamin A (retinol), and have been
214 a role of endogenous retinoic acid (RA), the active metabolite of vitamin A in the initial differenti
215 herein that all-trans-retinoic acid (RA), an active metabolite of vitamin A that is known to induce m
218 tem (CNS) the function of retinoic acid, the active metabolite of vitamin A, is best understood from
219 Retinoic acid (RA), the main biologically active metabolite of vitamin A, is known to promote gut
220 effect of all-trans retinoic acid (ATRA), an active metabolite of vitamin A, on the neuropathology an
222 All-trans-retinoic acid (atRA), the major active metabolite of vitamin A, plays a role in many bio
230 droxyvitamin D(3)(1alpha,25(OH)(2)D(3)), the active metabolite of vitamin D(3), mediates anti-prolife
231 ihydroxyvitamin D(3) [1, 25(OH)(2)D(3)], the active metabolite of vitamin D(3), on angiogenesis by us
233 study, we hypothesized that the biologically active metabolite of vitamin D, 1,25(OH)2D3, inhibits hu
237 rmone (VDH; 1,25-dihydroxyvitamin D(3)), the active metabolite of vitamin D, is the major Ca(2+)-regu
238 amin D3 (1alpha,25(OH)2D3), the biologically active metabolite of vitamin D3 To further investigate t
239 1,25-Dihydroxyvitamin D3 [1,25(OH)2D3], the active metabolite of vitamin D3, inhibits the proliferat
241 iously we demonstrated that the biologically active metabolites of 17beta-oestradiol, 2-hydroxyoestra
242 op1cc in biochemical assays, we propose that active metabolites of 4NQO trap Top1cc by forming DNA ad
243 We now report the synthesis of suspected active metabolites of BcF, specifically the trans-3,4-di
245 A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM and endoxifen, is by
246 etramethyl tetralin (1,2-DATT), the putative active metabolites of the neurotoxic aromatic hydrocarbo
247 provide comparable systemic exposure to the active metabolites of the prior, stable tetrabenazine re
248 ing compounds for the synthesis of the other active metabolites of these PAHs thought to be involved
250 ts produce an enormous array of biologically active metabolites, often with stereochemical variations
251 the peak plasma concentration of clopidogrel active metabolite (omeprazole > esomeprazole > lansopraz
252 Plasma concentrations of CI-1040 and its active metabolite, PD 0184264, increased in a less than
255 logic profile and its ability to deliver two active metabolites, potentially simplifying HCV treatmen
256 cessed by dendritic cells and T cells to the active metabolite, providing a mechanism for the local r
257 the high functional versatility of the redox-active metabolite pyocyanin and the susceptibility of ar
262 tration to mice and Wistar rats generated an active metabolite recovered from the rodent's brains.
264 ssential: they process the vitamins to their active metabolites (retinoic acid and 1,25(OH)(2)D3) for
265 is known about the role of vitamin A and its active metabolite, retinoic acid (RA) in host defenses a
267 ral levels of the prodrug irinotecan and its active metabolite SN-38 compared with free irinotecan.
268 ed PEG conjugates of the irinotecan (CPT-11) active metabolite SN-38 via a phenyl ether that release
272 ntrations of tenofovir, emtricitabine, their active metabolites (tenofovir diphosphate [TFVdp] and em
274 umatic fluorescent drug leflunomide into its active metabolite teriflunomide through isoxazole ring o
275 Because of a wide inter-patient range of active metabolite terminal half-life (>300%), monitoring
276 lized in rats, but MDC is the only centrally active metabolite that could contribute to overall effec
277 50 (CYP) metabolic activation to produce the active metabolite that inhibits the platelet P2Y(1)(2) a
278 l molecules would benefit the study of redox-active metabolites that are produced by microbial biofil
279 h agents undergo intracellular processing to active metabolites that disrupt RNA and DNA metabolism.
280 Clopidogrel is a prodrug anticoagulant with active metabolites that irreversibly inhibit the platele
281 s that PAHs are transformed enzymatically to active metabolites that react with DNA to form adducts t
282 lism leads to the generation of biologically active metabolites that regulate cell growth and prolife
283 oA modulating the generation of biologically active metabolites that regulate mitochondrial bioenerge
284 d that vitamin A, retinol, functions through active metabolites: the visual chromophore 11-cis-retina
285 an inactive prodrug; it is converted to its active metabolite through the cytochrome P450 (CYP3A4) p
286 eportedly reduce clopidogrel's metabolism to active metabolite, thus attenuating its inhibition of pl
289 is a novel prodrug formulated to deliver the active metabolite to target cells more efficiently than
290 vir impairs the conversion of 25(OH)D to the active metabolite, utilization of 25(OH)D may have been
292 ationship suggested the presence of a common active metabolite which may preclude this series of comp
293 ch has been focused on the identification of active metabolites, which are crucial for selenium chemo
294 both the parent compound ranolazine and its active metabolites, which have shown potent blocking eff
296 pedunculata studied is a potential source of active metabolites with a positive effect on human healt
297 resuscitation to promote renal excretion of active metabolite, withholding the doses and timely mana
298 ical models by enhancing accumulation of its active metabolite within the tumor microenvironment.
299 their abilities to convert amifostine to its active metabolite WR-1065, amifostine may not only prote
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