{
  "abstract": "Estrogen receptor alpha (ERα) is an important molecular target for the diagnosis and endocrine therapy of breast cancer. BHPI is a recently identified class of novel non-steroidal ERα-targeting small molecules; however，no studies on its radiolabeling or molecular imaging applications have been reported to date. In this study，a boronic ester precursor of BHPI (B-BHPI) was designed and synthesized，and the PET molecular probe 18F-BHPI was successfully prepared via a copper-mediated nucleophilic radiofluorination strategy. The radiochemical properties, in vitro stability，cellular uptake characteristics，and in vivo biodistribution of the probe were systematically evaluated. The results showed that 18F-BHPI was obtained with a radiochemical conversion (RCC) of (37.75±7.39)%，a radiochemical yield (RCY) of (6.28±0.15)%，a radiochemical purity (RCP) of (96.38±1.62)%，and a molar activity of (0.29±0.11) GBq/μmol. The LogP value was 1.10±0.27. The probe exhibited excellent stability in both saline and mouse serum，remaining predominantly intact after 240 min of incubation. Cellular uptake studies demonstrated significantly higher accumulation of 18F-BHPI in ERα-positive MCF-7 cells than in ERα-negative MDA-MB-231 cells. Competitive inhibition experiments further revealed that tamoxifen，17β-estradiol，and BHPI markedly reduced probe uptake in MCF-7 cells，with BHPI showing the strongest blocking effect. Biodistribution studies in normal female SD rats indicated that 18F-BHPI was mainly metabolized through the hepatobiliary and intestinal pathways and displayed a well-defined in vivo distribution and clearance profile. To the best of our knowledge，this study represents the first successful radiolabeling of BHPI and the first construction of a BHPI-based molecular imaging probe. The resulting 18F-BHPI exhibited favorable physicochemical properties and ERα-related uptake characteristics，providing a useful tool for in vivo tracing of BHPI and a promising foundation for the development of novel ERα-related PET molecular probes.",
  "abstract_shown": true,
  "affiliations": [
    "Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen 361003, China",
    "School of Public Health, Xiamen University, Xiamen 361102, China"
  ],
  "article_type": null,
  "arxiv": null,
  "author_total": 6,
  "authors": [
    {
      "affs": [
        0
      ],
      "name": "Yesen LI"
    },
    {
      "affs": [
        1
      ],
      "name": "Xueqi WANG"
    },
    {
      "affs": [
        1
      ],
      "name": "Yike WANG"
    },
    {
      "affs": [
        0
      ],
      "name": "Yuejing DENG"
    },
    {
      "affs": [
        1
      ],
      "name": "Xinying ZENG"
    },
    {
      "affs": [
        0
      ],
      "name": "Zhide GUO"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/8j1wt4vw9d7v4.bib",
  "cited_by": 0,
  "doi": "10.7538/tws.2026.youxian.057",
  "fulltext_url": "https://tws.xml-journal.net/article/doi/10.7538/tws.2026.youxian.057",
  "id": "8j1wt4vw9d7v4",
  "issns": [
    "1000-7512"
  ],
  "landing_url": "https://doi.org/10.7538/tws.2026.youxian.057",
  "language": "zh",
  "licence": "CC-BY-NC-ND",
  "licence_label": "CC BY-NC-ND",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by-nc-nd/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "lcc",
      "QC770-798"
    ],
    [
      "openalex",
      "2741|Radiopharmaceutical Chemistry and Applications"
    ]
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  "openalex": "W7224116501",
  "pdf_url": null,
  "pmcid": null,
  "pmid": null,
  "published": "2026-10-26",
  "publisher": "Editorial Board of Journal of Isotopes",
  "ris": "https://research.draconitic.com/paper/8j1wt4vw9d7v4.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T13:47:13Z",
      "native_id": "170ec43ec84d48de89428e161fcbffc1",
      "source": "doaj",
      "url": "https://doi.org/10.7538/tws.2026.youxian.057"
    }
  ],
  "subjects": [
    {
      "field": "medicine",
      "origin": "openalex:2741|Radiopharmaceutical Chemistry and Applications",
      "subfield": "imaging"
    }
  ],
  "title": "Preparation and Preliminary Evaluation of 18F-BHPI as a Novel PET Probe Targeting Estrogen Receptor Alpha (ERα)",
  "title_text": "Preparation and Preliminary Evaluation of 18F-BHPI as a Novel PET Probe Targeting Estrogen Receptor Alpha (ERα)",
  "type": "peer-reviewed",
  "updated_at": "2026-10-31T14:21:06Z",
  "url": "https://research.draconitic.com/paper/8j1wt4vw9d7v4",
  "venue": "Journal of Isotopes",
  "versions": []
}