40 years later: completion of the structural characterization of the anxiolytic drug buspirone HCl and solid-form landscape expansion
4 affiliations
- 1Department of Chemistry, University of Missouri 601 S. College Avenue Columbia MO 65211 USA
- 2Department of Chemistry and Biochemistry, Texas Tech University 1204 Boston Avenue Lubbock TX 79409 USA
- 3Rigaku Americas Corporation 9009 New Trails Dr The Woodlands TX 77381 USA
- 4MU Materials Science & Engineering Institute, University of Missouri Columbia MO 65211 USA
Abstract
Buspirone (Bus) is an anxiolytic drug and was commercialized forty years ago as an HCl salt. The HCl salt of Bus is also polymorphic, and here, using electron diffraction, we reveal the structure of Bus·HCl Form 2 for the first time. We also prepared the first multicomponent solids of Bus, and describe 15 solids, including cocrystals, an ionic cocrystal, and salts. Significant differences in the solid-state conformation of Bus are described, as well as impacts to the thermal properties upon incorporation into multicomponent solids. Bus, like many drug molecules, does not include a classic ionizable group, which could hamper solid-state development. Bus does include a piperazine ring, one of the five most frequently used nitrogen-based heterocycles in US FDA approved drugs, and is a key site for forming intermolecular hydrogen bonds in each solid. The strategies here could be applied to modify properties in other piperazine-containing drugs.
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BibTeX
@article{botes2026years,
title = {{40 years later: completion of the structural characterization of the anxiolytic drug buspirone HCl and solid-form landscape expansion}},
author = {Delbert S. Botes and Mikaela I. Aleman and Alyssa M. Anderson and Pierre Le Maguerès and Kristin M. Hutchins},
journal = {RSC advances},
year = {2026},
month = oct,
doi = {10.1039/d6ra07954g},
url = {https://europepmc.org/article/PMC/PMC13660027},
note = {CC BY-NC},
}
RIS
TY - JOUR
TI - 40 years later: completion of the structural characterization of the anxiolytic drug buspirone HCl and solid-form landscape expansion
AU - Delbert S. Botes
AU - Mikaela I. Aleman
AU - Alyssa M. Anderson
AU - Pierre Le Maguerès
AU - Kristin M. Hutchins
PY - 2026
DA - 2026/10/13
JO - RSC advances
DO - 10.1039/d6ra07954g
UR - https://europepmc.org/article/PMC/PMC13660027
AB - Buspirone (Bus) is an anxiolytic drug and was commercialized forty years ago as an HCl salt. The HCl salt of Bus is also polymorphic, and here, using electron diffraction, we reveal the structure of Bus·HCl Form 2 for the first time. We also prepared the first multicomponent solids of Bus, and describe 15 solids, including cocrystals, an ionic cocrystal, and salts. Significant differences in the solid-state conformation of Bus are described, as well as impacts to the thermal properties upon incorporation into multicomponent solids. Bus, like many drug molecules, does not include a classic ionizable group, which could hamper solid-state development. Bus does include a piperazine ring, one of the five most frequently used nitrogen-based heterocycles in US FDA approved drugs, and is a key site for forming intermolecular hydrogen bonds in each solid. The strategies here could be applied to modify properties in other piperazine-containing drugs.
SN - 2046-2069
ER -