Effects of metaphit on phencyclidine and serotonin2 receptors.
We have investigated whether metaphit, a derivative of phencyclidine (PCP) which irreversibly binds to a population of PCP receptor sites in rat brain, blocks PCP-induced head-twitch response which is produced through serotonin2 (5-HT2) receptors, and also whether metaphit decreases the capacity of 5-HT2 receptors. Metaphit (1 mumol/rat) had decreased the intensity of PCP-induced head-twitch response and had depleted both PCP and 5-HT2 receptors by 24 h after administration, but it failed to block 5-HT agonist 5-methoxy-N,N-dimethyltryptamine-induced 5-HT1A receptor-dependent behaviors. These results reconfirmed our hypothesis that PCP and 5-HT2 receptors may have very similar binding sites.
Nabeshima
T
T
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Meijo University, Nagoya, Japan.
Tohyama
K
K
Noda
A
A
Maeda
Y
Y
Hiramatsu
M
M
Harrer
S M
SM
Kameyama
T
T
Furukawa
H
H
Jacobson
A E
AE
Rice
K C
KC
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D007650:Ketanserin / Q000378:metabolism; D008297:Male; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011916:Rats, Inbred F344; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D017478:Receptors, Phencyclidine; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D013997:Time Factors
D017981:Receptors, Neurotransmitter; D017478:Receptors, Phencyclidine; D011985:Receptors, Serotonin; C044705:metaphit; D007650:Ketanserin; D010622:Phencyclidine