Synthesis and structure-activity relationship studies of theophylline analogs on population responses in the rat hippocampus in vitro.
We synthesized several theophylline analogs and tested the hypothesis that these compounds may be nootropic or cognitive enhancers by examining their effects on evoked population spikes recorded extracellularly in the CA1 region of the rat hippocampus. Whereas the length of the carbon chain on N7 had no effect, different size of the terminal lactam ring strongly influenced neuroactivity. Our results suggest that hexahydroazepin-2-one analogs have potential for further development as cognitive enhancers.
Ananthalakshmi
Kethireddy V V
KV
Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait.
Bartl
Tomás
T
Aziza
Mohammed H
MH
Novotný
Ladislav
L
Marek
Radek
R
Benes
Ludek
L
Kombian
Samuel B
SB
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004566:Electrodes; D006624:Hippocampus / Q000166:cytology / Q000187:drug effects* / Q000502:physiology; D008297:Male; D015394:Molecular Structure; D009474:Neurons / Q000145:classification / Q000187:drug effects* / Q000502:physiology; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013806:Theophylline / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D013997:Time Factors
D018697:Nootropic Agents; D013806:Theophylline