Brain serotonin receptors as a target for the putative anxiolytic TVX Q 7821.
In animal behavioral tests of anxiolytic efficacy, TVX Q 7821 was active and equipotent with diazepam, but did not produce muscle relaxation or anti-convulsant effects. The high affinity, specific binding of 3H-TVX Q 7821 to calf hippocampal membranes was displaced by serotonin (5-HT) but not by diazepam. Similarly, unlabeled TVX Q 7821 displaced 3H-5-HT but not 3H-flunitrazepam binding. Since ketanserin (a putative 5-HT2 ligand) was equally weak in displacing labeled 5-HT or TVX Q 7821, TVX Q 7821 may preferentially bind to 5-HT1, receptors.
D000374:Aggression / Q000187:drug effects; D000698:Analgesia; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D003975:Diazepam / Q000494:pharmacology; D004597:Electroshock; D005445:Flunitrazepam / Q000378:metabolism; D006801:Humans; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011743:Pyrimidines / Q000378:metabolism / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism
D011743:Pyrimidines; D011985:Receptors, Serotonin; D012701:Serotonin; D005445:Flunitrazepam; C043077:ipsapirone; D003975:Diazepam