Bupivacaine Analogue Toxicity and Pharmacokinetics in Mice and Guinea Pigs

Three spirocyclic analogues of the local anesthetic bupivacaine demonstrated 1.3-, 2.2-, and 5.0-fold increases in lethal dose in mice. This dataset, uploaded by Alexander A. Kirichok to figshare in 2026, contains results from animal studies and pharmacokinetic analysis comparing the toxicity and tissue affinity of these drug candidates.

Use Cases

• Compare cardiotoxicity levels based on QRS widening data from isolated guinea pig hearts mentioned in the description
• Analyze structure-activity relationships based on the replacement of the piperidine ring with spirocyclic scaffolds
• Model pharmacokinetic distribution based on relative affinity to plasma, brain, and heart tissues in mice
• Rank candidate compounds based on the reported increases in lethal dose (LD) values

Strengths

• Includes specific quantitative toxicity results: 1.3-, 2.2-, and 5.0-fold increases in lethal dose for three tested structures.
• Contains comparative pharmacokinetic data on tissue affinity (plasma vs. brain/heart).
• Dataset is small (1.6 KB), facilitating quick inspection and download.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• Data may reflect bias inherent to the specific animal models (mice, guinea pigs) used.

Provenance

Source

figshare

Collection Method

Likely contains experimental results from animal studies (mice, guinea pigs) and pharmacokinetic analysis.

Freshness

Last updated 2026-05-08 13:37:04; freshness should be verified.