Novel approaches, drug candidates, and targets in pain drug discovery

S Obeng, T Hiranita, F León, LR McMahon… - Journal of medicinal …, 2021 - ACS Publications
Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …

An update on the clinical pharmacology of kratom: uses, abuse potential, and future considerations

CR McCurdy, A Sharma, KE Smith… - Expert Review of …, 2024 - Taylor & Francis
ABSTRACT Introduction Kratom (Mitragyna speciosa) has generated substantial clinical and
scientific interest as a complex natural product. Its predominant alkaloid mitragynine and …

Activity of Mitragyna speciosa (“Kratom”) Alkaloids at Serotonin Receptors

F León, S Obeng, M Mottinelli, Y Chen… - Journal of medicinal …, 2021 - ACS Publications
Kratom alkaloids have mostly been evaluated for their opioid activity but less at other targets
that could contribute to their physiological effects. Here, we investigated the in vitro and in …

Examining the paradoxical effects of kratom: a narrative inquiry

KE Smith, JD Feldman, KE Dunn… - Frontiers in …, 2023 - frontiersin.org
Introduction: Surveys and case reports have documented kratom use in the United States
(US) for over a decade. However, those reports have generally not examined in depth the …

Oxidative metabolism as a modulator of kratom's biological actions

S Chakraborty, R Uprety, ST Slocum, T Irie… - Journal of medicinal …, 2021 - ACS Publications
The leaves of Mitragyna speciosa (kratom), a plant native to Southeast Asia, are increasingly
used as a pain reliever and for attenuation of opioid withdrawal symptoms. Using the tools of …

Exploring the Chemistry of Alkaloids from Malaysian Mitragyna speciosa (Kratom) and the Role of Oxindoles on Human Opioid Receptors

NJY Chear, F León, A Sharma… - Journal of natural …, 2021 - ACS Publications
Ten indole and oxindole alkaloids (1–10) were isolated from the freshly collected leaves of
Malaysian Mitragyna speciosa (Kratom). The chemical structures of these compounds were …

Clinical Pharmacokinetic Assessment of Kratom (Mitragyna speciosa), a Botanical Product with Opioid-like Effects, in Healthy Adult Participants

RS Tanna, JT Nguyen, DL Hadi, PK Manwill… - Pharmaceutics, 2022 - mdpi.com
Increasing use of the botanical kratom to self-manage opioid withdrawal and pain has led to
increased kratom-linked overdose deaths. Despite these serious safety concerns, rigorous …

A novel mitragynine analog with low-efficacy mu opioid receptor agonism displays antinociception with attenuated adverse effects

S Chakraborty, JF DiBerto, A Faouzi… - Journal of medicinal …, 2021 - ACS Publications
Mitragynine and 7-hydroxymitragynine (7OH) are the major alkaloids mediating the
biological actions of the psychoactive plant kratom. To investigate the structure–activity …

Searching for a signal: self-reported kratom dose-effect relationships among a sample of US adults with regular kratom use histories

KE Smith, JM Rogers, KE Dunn… - Frontiers in …, 2022 - frontiersin.org
There is limited understanding regarding kratom use among US adults. Although
motivations for use are increasingly understood, typical kratom doses, threshold of (low and …

Accelerated Solvent Extractions (ASE) of Mitragyna speciosa Korth. (Kratom) Leaves: Evaluation of Its Cytotoxicity and Antinociceptive Activity

YS Goh, T Karunakaran, V Murugaiyah, R Santhanam… - Molecules, 2021 - mdpi.com
Mitragyna speciosa Korth (kratom) is known for its psychoactive and analgesic properties.
Mitragynine is the primary constituent present in kratom leaves. This study highlights the …