The influence of lipophilic character on receptor binding affinity of a series of beta-carbolines.
A quantitative study of the relationship between structure and receptor binding affinity of a series of 16 beta-carbolines showed the influence of lipophilic character and hydrogen bonding capability of substituents in position 3. Some data taken from the literature enabled us to add some evidence about the influence of planarity of ring C and bulky substituents in position 1 in determining the receptor binding affinity.
Borea
P A
PA
Istituto di Farmacologia, Universita di Ferrara, Italy.
Pietrogrande
M C
MC
Biagi
G L
GL
D000818:Animals; D002243:Carbolines / Q000378:metabolism*; D006860:Hydrogen Bonding; D066298:In Vitro Techniques; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D012995:Solubility; D013329:Structure-Activity Relationship
D002243:Carbolines; D011963:Receptors, GABA-A