BPR1M492: Structural Modification Data for a Potent Opioid Analgesic

A series of N-(1,2,3,4-tetrahydro-3-isoquinolinylmethyl)benzamides, potent μ-opioid receptor agonists, has been discovered. The most promising compound, BPR1M492, demonstrated potent in vivo antinociception at 0.027 mg/kg, offering rapid pain relief within 5 minutes of subcutaneous injection. The dataset was authored by Po-Wei Chang and last updated on June 1, 2026.

Use Cases

• Structure-activity relationship (SAR) analysis based on the series of benzamide derivatives described.
• Comparative efficacy studies against other analgesics like TRV130 based on reported antinociception dose and withdrawal symptom data.
• Investigating signaling bias in opioid receptor pathways based on the description of cAMP and β-arrestin-2 pathway activity.
• Preclinical safety assessment based on the compound's described stability, hygroscopicity, and safety at effective dose.

Strengths

• Dataset includes specific, quantitative efficacy data: potent antinociception at 0.027 mg/kg.
• Provides comparative data on withdrawal symptoms versus TRV130, a known benchmark.
• Describes key physicochemical properties: highly stable, slightly hygroscopic, low-moisture crystalline solid.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Description metadata is limited; actual data quality requires manual inspection after download.

Provenance

Source

figshare

Freshness

Last updated 2026-06-01 19:38:43; freshness should be verified.