Pub. Date : 2013 Sep
PMID : 23822584
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | KEY RESULTS: Dopamine, quipazine and VUF10166 were partial agonists at wild type 5-HT3A and 5-HT3AB receptors, with quipazine and VUF10166 causing a long-lived (>20 min) inhibition of subsequent agonist responses. | Quipazine | 5-hydroxytryptamine receptor 3A | Homo sapiens |
| 2 | A T6"S substitution in the 5-HT3A subunit decreased EC50 and increased Rmax of dopamine and quipazine at both homomeric and heteromeric receptors. | Quipazine | 5-hydroxytryptamine receptor 3A | Homo sapiens |
| 3 | CONCLUSIONS AND IMPLICATIONS: These results indicate that a mutation in the pore lining domain in both 5-HT3A and 5-HT3AB receptors alters the relative efficacy of a series of agonists, changing some (e.g. quipazine) from apparent antagonists to potent and efficacious agonists. | Quipazine | 5-hydroxytryptamine receptor 3A | Homo sapiens |