Tesi etd-02132021-101354 |
Link copiato negli appunti
Tipo di tesi
Tesi di laurea magistrale LM5
Autore
RICARDI, CATERINA
URN
etd-02132021-101354
Titolo
Cannabinoid CB2 receptor modulators in the treatment of rheumatoid arthritis and osteoarthritis
Dipartimento
FARMACIA
Corso di studi
CHIMICA E TECNOLOGIA FARMACEUTICHE
Relatori
relatore Prof.ssa Manera, Clementina
relatore Dott.ssa Ferrisi, Rebecca
relatore Dott. Lowin, Torsten
relatore Dott.ssa Ferrisi, Rebecca
relatore Dott. Lowin, Torsten
Parole chiave
- cannabinoid
- cannabinoid cb1 receptor
- cannabnoid cb2 receptor
- endocannabinoid system
- osteoarthritis
- rheumatic disease
- rheumatoid arthritis
Data inizio appello
03/03/2021
Consultabilità
Completa
Riassunto
Rheumatoid arthritis (RA) and osteoarthritis (OA) are two common types of arthritis, both characterized by pain and joint damage.
Current treatment options for RA and OA are not always optimal, and long-term use of some medications leads to several side effects. Thus, identification of novel therapeutic agents with fewer drawbacks for the treatment of RA and OA is needed. One drug target that may have a role in the modulation of pain and inflammation associated with these rheumatic diseases is the endocannabinoid system (ECS).
Generally, the ECS activation, has shown efficacy in experimental models of RA and OA. Specific activation of CB2R could lead to an immunomodulatory and anti-inflammatory effect, thus relieving RA and OA. In parallel, the activation of CB1R may lead to an antinociceptive effect and could reduce the sympathetic nervous system and its neurotransmitters, thus counteracting the comorbidities which often accompany the RA disease.
In my thesis work, I synthesized three well-characterized CBRs active ligands, in order to evaluate their immunomodulatory and anti-inflammatory effects on the RA and OA in vitro models: EC21a is the first positive allosteric modulator at CB2R; FM6b is a dual orthosteric agonist at CB1R and CB2R; LV62 is a highly selective CB2R agonist. These assays are ongoing at the University Hospital of Dusseldorf in research lab of Professor Pongratz and Dr. Torsten Lowin.
Current treatment options for RA and OA are not always optimal, and long-term use of some medications leads to several side effects. Thus, identification of novel therapeutic agents with fewer drawbacks for the treatment of RA and OA is needed. One drug target that may have a role in the modulation of pain and inflammation associated with these rheumatic diseases is the endocannabinoid system (ECS).
Generally, the ECS activation, has shown efficacy in experimental models of RA and OA. Specific activation of CB2R could lead to an immunomodulatory and anti-inflammatory effect, thus relieving RA and OA. In parallel, the activation of CB1R may lead to an antinociceptive effect and could reduce the sympathetic nervous system and its neurotransmitters, thus counteracting the comorbidities which often accompany the RA disease.
In my thesis work, I synthesized three well-characterized CBRs active ligands, in order to evaluate their immunomodulatory and anti-inflammatory effects on the RA and OA in vitro models: EC21a is the first positive allosteric modulator at CB2R; FM6b is a dual orthosteric agonist at CB1R and CB2R; LV62 is a highly selective CB2R agonist. These assays are ongoing at the University Hospital of Dusseldorf in research lab of Professor Pongratz and Dr. Torsten Lowin.
File
Nome file | Dimensione |
---|---|
TesiCate...cardi.pdf | 7.25 Mb |
Contatta l’autore |