sigma receptors in rat brain and testes show similar reductions in response to chronic haloperidol.
The effect of haloperidol upon [3H]1,3-di-o-tolylguanidine ([3H]DTG) binding sites was assessed in rat brain and testes. An acute injection (10 mg/kg), in rats culled 2 h later, changed Kd values from 18 +/- 2 to 108 +/- 26 nM (brain) and 14 +/- 1 to 116 +/- 35 nM (testes), with unchanged Bmax values. Rats were injected with 4 mg/kg per day for 7, 14 and 21 days and culled 4 days after the last injection. By day 21, there was an average fall in Bmax for brain of 30% and for testes of 38%. Kd values remained unchanged. Thus peripheral and central [3H]DTG binding sites were reduced by chronic haloperidol in a similar way.
Jansen
K L
KL
Oxford University Clinical Pharmacology Department, Radcliffe Infirmary, U.K.
Elliot
M
M
Leslie
R A
RA
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006146:Guanidines / Q000378:metabolism; D006220:Haloperidol / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D009928:Organ Specificity; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism; D017480:Receptors, sigma; D013737:Testis / Q000187:drug effects / Q000378:metabolism
D006146:Guanidines; D011957:Receptors, Opioid; D017480:Receptors, sigma; D006220:Haloperidol; C050232:1,3-ditolylguanidine