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Preparation and Delivery of Protein Microcrystals in Lipidic Cubic Phase for Serial Femtosecond Crystallography
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Studies To Examine Potential Tolerability Differences between the 5-HT2C Receptor Selective Agonists Lorcaserin and

Guy A Higgins1,2, Leonardo B Silenieks1, Amy Patrick1

  • 1InterVivo Solutions Inc. , 120 Carlton Street, Toronto, Ontario M5A 4K2, Canada.

ACS Chemical Neuroscience
|March 25, 2017
PubMed
Summary

Lorcaserin (LOR) and CP-809101 (CP) are 5-HT2C agonists for obesity. CP shows better tolerability due to limited central nervous system (CNS) levels at higher doses, unlike LOR.

Keywords:
5-HTCP-809101CSF compartmentSerotoninbiased signalingconditioned gapingdrug discriminationlorcaserinnauseapharmacokineticsplasma compartmentrat

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Development

Background:

  • Lorcaserin (LOR) is an FDA-approved 5-HT2C receptor agonist for obesity treatment.
  • Nausea and headache are common dose-limiting side effects of LOR.
  • Previous studies suggested CP-809101 (CP), a selective 5-HT2C agonist, may have better tolerability than LOR.

Purpose of the Study:

  • Investigate the differing tolerability between LOR and CP.
  • Identify potential mechanisms underlying the observed side effect differences.
  • Explore pharmacokinetic and signaling pathway variations between the two agonists.

Main Methods:

  • Utilized a conditioned gaping model in rats to assess emetogenic properties.
  • Conducted drug discrimination studies to evaluate interoceptive cues.
  • Performed in vitro functional selectivity assays in CHO cells expressing h5-HT2C receptors.
  • Analyzed drug plasma and cerebrospinal fluid (CSF) levels in rats.

Main Results:

  • LOR induced significantly more conditioned gapes than CP, indicating higher emetogenic potential.
  • Both LOR and CP produced full generalization in drug discrimination, suggesting similar interoceptive cues.
  • In vitro assays revealed no biased signaling differences between LOR and CP across PLC, PLA2, and ERK pathways.
  • CSF levels of LOR increased proportionally with dose, while CP's CSF levels plateaued at higher doses.

Conclusions:

  • The improved tolerability of CP compared to LOR is likely due to dose-dependent limitations in its central nervous system (CNS) penetration.
  • Despite similar in vitro signaling and interoceptive cues, pharmacokinetic differences contribute to varying side effect profiles.
  • Understanding these pharmacokinetic-pharmacodynamic relationships is crucial for developing better-tolerated anti-obesity medications.