Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action.
Animals
Sumatriptan
/ pharmacokinetics
Tryptamines
/ pharmacokinetics
Rats
Male
Rats, Sprague-Dawley
Blood-Brain Barrier
/ drug effects
Pyrrolidines
/ pharmacokinetics
Serotonin Receptor Agonists
/ pharmacokinetics
Peripheral Nervous System
/ drug effects
Central Nervous System
/ metabolism
Serotonin 5-HT1 Receptor Agonists
/ pharmacology
Receptors, Serotonin
/ metabolism
Receptor, Serotonin, 5-HT1D
/ metabolism
Receptor, Serotonin, 5-HT1B
/ metabolism
Brain
/ metabolism
Tissue Distribution
/ drug effects
Trigeminal Ganglion
/ metabolism
5-HT1B/1D/1F receptors
Blood-brain barrier
CNS
Central effect
Combinatory mapping approach
Eletriptan
Free drug theory
Migraine
PNS
Sumatriptan
Journal
The journal of headache and pain
ISSN: 1129-2377
Titre abrégé: J Headache Pain
Pays: England
ID NLM: 100940562
Informations de publication
Date de publication:
30 Oct 2024
30 Oct 2024
Historique:
received:
01
10
2024
accepted:
22
10
2024
medline:
31
10
2024
pubmed:
31
10
2024
entrez:
31
10
2024
Statut:
epublish
Résumé
Triptans are potent 5-HT Using the Combinatory Mapping Approach (CMA) for regions of interest (ROI), we assessed the unbound tissue-to-plasma concentration ratio (K We observed heterogenous triptan transport across CNS and PNS regions with the highest extent of unbound drug transport across the blood-nerve barrier in the trigeminal ganglion (K This study suggests that despite low BBB transport, both eletriptan and sumatriptan achieve unbound concentrations sufficient to stimulate 5-HT
Sections du résumé
BACKGROUND
BACKGROUND
Triptans are potent 5-HT
METHODS
METHODS
Using the Combinatory Mapping Approach (CMA) for regions of interest (ROI), we assessed the unbound tissue-to-plasma concentration ratio (K
RESULTS
RESULTS
We observed heterogenous triptan transport across CNS and PNS regions with the highest extent of unbound drug transport across the blood-nerve barrier in the trigeminal ganglion (K
CONCLUSIONS
CONCLUSIONS
This study suggests that despite low BBB transport, both eletriptan and sumatriptan achieve unbound concentrations sufficient to stimulate 5-HT
Identifiants
pubmed: 39478486
doi: 10.1186/s10194-024-01894-0
pii: 10.1186/s10194-024-01894-0
doi:
Substances chimiques
Sumatriptan
8R78F6L9VO
eletriptan
22QOO9B8KI
Tryptamines
0
Pyrrolidines
0
Serotonin Receptor Agonists
0
Serotonin 5-HT1 Receptor Agonists
0
Receptors, Serotonin
0
Receptor, Serotonin, 5-HT1D
0
Receptor, Serotonin, 5-HT1B
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
187Subventions
Organisme : Innovative Medicines Initiative 2 Joint Undertaking
ID : 807015
Organisme : Innovative Medicines Initiative 2 Joint Undertaking
ID : 807015
Organisme : Innovative Medicines Initiative 2 Joint Undertaking
ID : 807015
Organisme : Innovative Medicines Initiative 2 Joint Undertaking
ID : 807015
Informations de copyright
© 2024. The Author(s).
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