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Record W2326802383 · doi:10.1021/jm2001162

Preparation, Characterization, and Screening of a High Affinity Organometallic Probe for α-Adrenergic Receptors

2011· article· en· W2326802383 on OpenAlexaff
Anika S. Louie, Neil Vasdev, John F. Valliant

Bibliographic record

VenueJournal of Medicinal Chemistry · 2011
Typearticle
Languageen
FieldMedicine
TopicRadiopharmaceutical Chemistry and Applications
Canadian institutionsCentre for Addiction and Mental HealthUniversity of TorontoMcMaster University
Fundersnot available
KeywordsChemistryReceptorAdrenergic receptorSerotoninAmide5-HT receptorStereochemistryAdrenergicBiochemistry

Abstract

fetched live from OpenAlex

An organometallic rhenium complex having high and selective affinity for α-adrenergic receptors is reported. A series of methoxyphenylpiperazinecarborane ligands complexed to the [Re(CO)(3)](+) core were prepared and the resulting organometallic compounds screened for binding to serotonin, σ, and adrenergic receptors as well as dopamine, serotonin, and norepinephrine transporters. An amide linked derivative, for which a single crystal X-ray structure was obtained, showed high and selective affinity toward α(1A), α(1D), and α(2C) adrenergic receptors with K(i) values of 17, 21, and 39 nM, respectively. A method to prepare the corresponding (99m)Tc complex was also developed where the resulting metallocarborane was shown to be stable and is therefore suitable for in vivo molecular imaging studies.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.011
Threshold uncertainty score0.421

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.042
GPT teacher head0.308
Teacher spread0.266 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations26
Published2011
Admission routes1
Has abstractyes

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