Reference

Pharmacodynamic effects of zopiclone

Pharmacodynamic effects of zopiclone. Tokunaga, Tuneo; Morishita, Hideji; Kushiku, Kazushi; Abe, Masayoshi; Matsuki, Junko; Inoue, Takato (Sch. Med., Fukuoka Univ., Fukuoka 814-01, Japan). Igaku Kenkyu, 53(4), 224-32 (Japanese) 1983. CODEN: IGKEAO. ISSN: 0076-597X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Zopiclone (I) [43200-80-2] (1 mg/kg, i.v.) slightly decreased the respiration and heart rate without affecting blood pressure and ECG. I (10-6 g/mL) had no effect on isolated guinea pig atria and small intestine. I (1-10 mg/kg, i.v.) had no effect on the in vivo rabbit intestinal movement. I (10-5 g/mL) did not induce hemolysis. Thus, I has a weak or no effect on the peripheral organs in various animals.

Brain receptors and zopiclone

Brain receptors and zopiclone. Blanchard, J. C.; Boireau, A.; Julou, L. (Cent. Nicolas Grillet, Rhone-Poulenc Rech., Vitry-sur-Seine F-94400, Fr.). Pharmacology, 27(Suppl. 2), 59-69 (English) 1983. CODEN: PHMGBN. ISSN: 0031-7012. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Zopiclone (ZPC) [43200-80-2], chem. unrelated to benzodiazepines (BZD), has a similar pharmacol. profile and exhibits in man hypnotic activity similar to that of some BZD such as nitrazepam. The interaction of ZPC with rat brain receptors and esp. with the BZD receptors was studied. ZPC possesses in 3 rat brain regions a high affinity for BZD receptors; its Ki values measured against flunitrazepam are 24 nM in the cerebral cortex, 31 nM in the cerebellum, and 36 nM in the hippocampus. No other brain receptors, such as those for GABA, dopamine, serotonin, and noradrenaline, are reached by ZPC. Moreover, ZPC seems to bind only to brain BZD receptors and, contrarily to some BZD such as flunitrazepam, it does not reach the peripheral renal BZD-binding sites. The high affinity of ZPC was confirmed by equil.-binding studies (KD = 13 nM in rat hippocampus). A study of the modulating effect of GABA and barbiturates on ZPC binding revealed some differences between ZPC and BZD. It could, therefore, be postulated that ZPC might bind to rat brain sites which do not correspond exactly with BZD sites.