| Assay Method Information | |
| | Binding of Neurotensin to the NTSR1 Receptor |
| Description: | Inhibition higher than 50% of a certain receptor radioligand in the presence of 30 micromolar GAL475 was observed with 5-HT2B(h) (agonist radioligand; 75%), 5-HT5a(h) (agonist radioligand; 50.6%), 5-HT7 (h) (agonist radioligand; 79%), al adrenoreceptor (non-selective) (antagonist radioligand; 67.1%) and Na+channel (site 2) (antagonist radioligand; 75.1%). However, the potency of GAL 475 at these receptors was lower than 1 micromolar and therefore not considered to be pharmacologically interesting. An unexpected finding was however that at 30 micromolar, GAL475 enhanced rather than inhibited NTS1 (h) (agonist radioligand) by 32% suggesting it to be a positive allosteric modulator (PAM). GAL475 was subsequently tested for PAM activity at the human NTS1 (FAST-0330I) and NTS2 (FAST-0331I) receptors, at 100-50,000 nanomolar concentrations. |
| Affinity data for this assay | |
|---|---|
| If you find an error in this entry please send us an E-mail | |