Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3.
Eur J Med Chem
; 46(1): 142-9, 2011 Jan.
Article
in En
| MEDLINE
| ID: mdl-21093118
ABSTRACT
A number of 4-aryl-5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine with 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indole or 2-methyl-3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indole residues were synthesized for further investigation of SAR in a group of pyrido[1,2-c]pyrimidine derivatives with dual 5-HT(1A)/SERT activity. Compounds 8a-8p were found to be potent ligands for both 5-HT(1A) and SERT with K(i) ranging from 28,3 to 642 nM and 42,4 nM-1,8 µM, respectively. Moreover compounds 8a, 8b, 8c, 8d, 8e and 8g were found to be selective agonists, while 8i as an antagonist of 5-HT(1A) presynaptic receptors in the inducible hypothermia test in mice.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrimidines
/
Selective Serotonin Reuptake Inhibitors
/
Receptor, Serotonin, 5-HT1A
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Serotonin 5-HT1 Receptor Agonists
/
Serotonin 5-HT1 Receptor Antagonists
Limits:
Animals
Language:
En
Journal:
Eur J Med Chem
Year:
2011
Document type:
Article
Affiliation country:
Polonia