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5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential
- Source :
- European journal of pharmacology. 420(2-3)
- Publication Year :
- 2001
-
Abstract
- To examine further the hypothesis that the magnitude of the intrinsic activity of agonists at 5-HT1A receptors determines the magnitude of their psychotropic activity, we studied the relationship between the maximal receptor activation produced by various 5-HT1A receptor ligands and their antidepressant-like effects (i.e., decreased immobility in the forced swimming test in rats). Using three different in vitro assays suitable to measure differences among high, intermediate, and low efficacy 5-HT1A receptor agonists, ligands were identified with intrinsic activities ranging from low-negative (i.e., the inverse agonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexane-carboxamide (WAY 100635)) to high-positive (i.e., 3-chloro-4-fluorophenyl-(4-fluoro-4-{[(5-methyl-6-methylamino-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone (F 13714)). In addition, novel compounds with intermediate intrinsic activity, like buspirone, but with high selectivity for 5-HT1A receptors, unlike buspirone, were identified. The maximal effects of the 5-HT1A receptor ligands in the forced swimming test correlated positively (rS=0.91, P
- Subjects :
- Agonist
Male
medicine.medical_specialty
Intrinsic activity
medicine.drug_class
Pyridines
Aminopyridines
Pharmacology
Biology
Motor Activity
Binding, Competitive
Piperazines
Buspirone
Rats, Sprague-Dawley
Radioligand Assay
Piperidines
Internal medicine
medicine
Cyclic AMP
Inverse agonist
Animals
Humans
Receptor
5-HT receptor
Swimming
8-Hydroxy-2-(di-n-propylamino)tetralin
Dose-Response Relationship, Drug
Colforsin
Biological activity
Antidepressive Agents
Rats
Serotonin Receptor Agonists
Endocrinology
Guanosine 5'-O-(3-Thiotriphosphate)
Receptors, Serotonin
5-HT1A receptor
Serotonin Antagonists
Receptors, Serotonin, 5-HT1
medicine.drug
HeLa Cells
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 420
- Issue :
- 2-3
- Database :
- OpenAIRE
- Journal :
- European journal of pharmacology
- Accession number :
- edsair.doi.dedup.....57bb419cb5f224370db3245d077cc08f