ArticleThe AAPS journal2022
Metabolism of Speciociliatine, an Overlooked Kratom Alkaloid for its Potential Pharmacological Effects.
Article in The AAPS journal, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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.
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Who cites it
17 citing papers in PubMed, 23 citations in OpenAlex.
- Assessment of Abuse Potential-Related Effects of Oral Dried Kratom Leaf Powder in Healthy Normal Participants Following Single and Multiple Daily Doses.Drug testing and analysis · 2026Trial
- Human Mitragynine and 7-Hydroxymitragynine Pharmacokinetics after Single and Multiple Daily Doses of Oral Encapsulated Dried Kratom Leaf Powder.Molecules (Basel, Switzerland) · 2024Trial
- Simultaneous quantification of seventeen kratom alkaloids and metabolites in human plasma and its application to clinical pharmacokinetic sample analysis.Pharmaceutical biology · 2026Article
- Avoiding False Identification of 7-Hydroxymitragynine in Kratom Products Using a Multicriteria LC-MS Confirmation.Journal of the American Society for Mass Spectrometry · 2026Article
- Characteristics of adverse reactions to kratom and implementation of harm reduction strategies in a sample of ethnobotanical tea bar patrons in Colorado.Harm reduction journal · 2026Article
- Mixtures Biotransformation: Multilayer Molecular Networking of Kratom Liver Metabolites.Journal of natural products · 2026Article
- Observational real-world analysis of dose-dependent effects ofFrontiers in pharmacology · 2026Article
- Comprehensive pharmacokinetics and ADME evaluation of Akuamma alkaloids.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2025Article
- In Vitro and In Vivo Pharmacokinetic Characterization of 7-Hydroxymitragynine, an Active Metabolite of Mitragynine, in Sprague-Dawley Rats.European journal of drug metabolism and pharmacokinetics · 2025Article
- Quantification of 11 kratom alkaloids including mitragynine and its main metabolites in human plasma using LC-MS/MS.Analytical and bioanalytical chemistry · 2025Article
- Article
- Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.Journal of medicinal chemistry · 2024Article
- Kratom safety and toxicology in the public health context: research needs to better inform regulation.Frontiers in pharmacology · 2024Review
- Growing pains with kratom: experiences discussed in subreddits contrast with satisfaction expressed in surveys.Frontiers in pharmacology · 2024Article
- Evaluating health information provided to kratom consumers by good manufacturing practice-qualified vendors.Substance abuse treatment, prevention, and policy · 2023Article
- Variations in mitragynine content in the naturally growing Kratom (Frontiers in plant science · 2022Article
- An update on the clinical pharmacology of kratom: uses, abuse potential, and future considerations.Expert review of clinical pharmacologyReview
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 1 country.
Funding
Abstract
Speciociliatine, a diastereomer of mitragynine, is an indole-based alkaloid found in kratom (Mitragyna speciosa). Kratom has been widely used for the mitigation of pain and opioid dependence, as a mood enhancer, and/or as an energy booster. Speciociliatine is a partial µ-opioid agonist with a 3-fold higher binding affinity than mitragynine. Speciociliatine has been found to be a major circulating alkaloid in humans following oral administration of a kratom product. In this report, we have characterized the metabolism of speciociliatine in human and preclinical species (mouse, rat, dog, and cynomolgus monkey) liver microsomes and hepatocytes. Speciociliatine metabolized rapidly in monkey, rat, and mouse hepatocytes (in vitro half-life was 6.6 ± 0.2, 8.3 ± 1.1, 11.2 ± 0.7 min, respectively), while a slower metabolism was observed in human and dog hepatocytes (91.7 ± 12.8 and > 120 min, respectively). Speciociliatine underwent extensive metabolism, primarily through monooxidation and O-demethylation metabolic pathways in liver microsomes and hepatocytes across species. No human-specific or disproportionate metabolites of speciociliatine were found in human liver microsomes. The metabolism of speciociliatine was predominantly mediated by CYP3A4 with minor contributions by CYP2D6.
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