Evidence map›Paper›PMID 25425116›Full record

ArticleEuropean journal of drug metabolism and pharmacokinetics2016

In vitro metabolism of bencycloquidium bromide and its inhibitory effects on human P450 isoenzymes: implication of CYP2D6, CYP2C19 and CYP3A4/5.

Janvier Engelbert Agbokponto, Lingling Zhang, Linlin Hu, Hao Feng, Li Ding

Abstract read
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In one paragraph

Article in European journal of drug metabolism and pharmacokinetics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.4field-weighted citation impact, top 30% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed, 4 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Janvier Engelbert AgbokpontoDepartment of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.
Lingling ZhangXenoBiotic Laboratories, Inc., Nanjing, 210038, China.
Linlin HuDepartment of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China.
Hao FengXenoBiotic Laboratories, Inc., Nanjing, 210038, China.
Li DingDepartment of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, China. dinglidl@hotmail.com.
China Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Bencycloquidium bromide (BCQB) is a novel selective muscarinic M1/M3 receptor antagonist with potent therapeutic effects on rhinitis and chronic obstructive pulmonary disease. The metabolism of BCQB has been investigated in human liver microsomes and human recombinant P450 to elucidate the P450 isozymes responsible for its metabolism in human. Also, the metabolism pathway and the potency of BCQB in inhibiting CYP's various isozymes in humans were investigated. The main biotransformation route of BCQB was NADPH-dependent oxidation. BCQB was metabolized oxidatively to four metabolites that were identified as monohydroxylated derivatives of BCQB at the phenyl and pentyl moieties of the molecule. The results from in vitro inhibition studies indicated that quinidine inhibited 86 % of metabolism of BCQB, while ticlopidine and ketoconazole inhibited 39 and 29 %, respectively. Inhibition studies with selective chemical inhibitors and incubations with human recombinant P450 isoforms demonstrated that the oxidative metabolism of BCQB is mediated by CYP2D6, CYP2C19 and CYP3A4/5, whereas BCQB had no inhibitory effect on any other P450 isoenzyme in humans.

Indexed as

Bridged Bicyclo Compounds, HeterocyclicCytochrome P-450 CYP2C19 InhibitorsCytochrome P-450 CYP2D6 InhibitorsCytochrome P-450 CYP3A InhibitorsDose-Response Relationship, DrugFemaleHumansIsoenzymesMaleMicrosomes, Liverbencycloquidium bromideBridged Bicyclo Compounds, HeterocyclicCytochrome P-450 CYP2C19 InhibitorsCytochrome P-450 CYP2D6 InhibitorsCytochrome P-450 CYP3A InhibitorsIsoenzymesBencycloquidium bromideDrug metabolismEnzymesHuman liver microsomesInhibitory effects

Identifiers

PMID25425116
OpenAlexW2046714227

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.