clozapine and benzamide

clozapine has been researched along with benzamide* in 2 studies

Other Studies

2 other study(ies) available for clozapine and benzamide

Article	Year
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. Bioorganic & medicinal chemistry letters, 2003, Mar-10, Volume: 13, Issue:5 Investigation of conformationally restricted benzamide bioisosteres led to the chiral phenyltetrahydropyrimidine derivative ent2a (FAUC 312) displaying strong and highly selective dopamine D4 receptor binding (K(i(high))=1.5 nM). Mitogenesis experiments indicated 83% ligand efficacy when compared to the unselective agonist quinpirole. The target compounds of type 2 and 3 were synthesized in enantiopure form starting from asparagine. Topics: Amidines; Animals; Benzamides; Cattle; CHO Cells; Clozapine; Cricetinae; Cyclization; Humans; Kinetics; Ligands; Mitogens; Mitosis; Piperazines; Pyrimidines; Quinpirole; Receptors, Dopamine D2; Receptors, Dopamine D4; Stereoisomerism; Structure-Activity Relationship	2003
How does the benzamide antipsychotic amisulpride get into the brain?--An in vitro approach comparing amisulpride with clozapine. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2003, Volume: 28, Issue:11 This study evaluated the disposition of the two atypical antipsychotics, amisulpride (AMS) and clozapine (CLZ), and its main metabolite N-desmethylclozapine (DCLZ), to their target structures in the central nervous system by applying an in vitro blood-brain barrier and blood-cerebrospinal fluid (CSF) barrier based on monolayers of porcine brain microvessel endothelial cells (PMEC) or porcine choroid plexus epithelial cells (PCEC). Permeation studies through PMEC- and PCEC-monolayers were conducted for 60 min at drug concentrations of 1, 5, 10, and 30 muM applied to the donor compartment. PMEC were almost impermeable for AMS (permeation coefficient, P<1 x 10(-7) cm/s) in the resorptive direction, whereas transport in the secretory direction was observed with a P (+/-SD) of 5.2+/-3.6 x 10(-6) cm/s. The resorptive P of CLZ and DCLZ were 2.3+/-1.2 x 10(-4) and 9.6+/-5.0 x 10(-5) cm/s, respectively. For the permeation across PCEC in the resorptive direction, a P of 1.7+/-2.5 x 10(-6) cm/s was found for AMS and a P of 1.6+/-0.9 x 10(-4) and 2.3+/-1.3 x 10(-5) cm/s was calculated for CLZ and DCLZ, respectively. Both, CLZ and DCLZ, could easily pass both barriers with about a five-fold higher permeation rate of CLZ at the PCEC. The permeation of AMS across the BBB was restricted partly due to an efflux transport. It is thus suggested that AMS reaches its target structures via transport across the blood-CSF barrier. Topics: Amisulpride; Animals; Antipsychotic Agents; Benzamides; Brain; Caco-2 Cells; Clozapine; Dose-Response Relationship, Drug; Humans; Sulpiride; Swine	2003

Article

Year

Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.

Bioorganic & medicinal chemistry letters, 2003, Mar-10, Volume: 13, Issue:5

Investigation of conformationally restricted benzamide bioisosteres led to the chiral phenyltetrahydropyrimidine derivative ent2a (FAUC 312) displaying strong and highly selective dopamine D4 receptor binding (K(i(high))=1.5 nM). Mitogenesis experiments indicated 83% ligand efficacy when compared to the unselective agonist quinpirole. The target compounds of type 2 and 3 were synthesized in enantiopure form starting from asparagine.

Topics: Amidines; Animals; Benzamides; Cattle; CHO Cells; Clozapine; Cricetinae; Cyclization; Humans; Kinetics; Ligands; Mitogens; Mitosis; Piperazines; Pyrimidines; Quinpirole; Receptors, Dopamine D2; Receptors, Dopamine D4; Stereoisomerism; Structure-Activity Relationship

2003

How does the benzamide antipsychotic amisulpride get into the brain?--An in vitro approach comparing amisulpride with clozapine.

Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2003, Volume: 28, Issue:11

This study evaluated the disposition of the two atypical antipsychotics, amisulpride (AMS) and clozapine (CLZ), and its main metabolite N-desmethylclozapine (DCLZ), to their target structures in the central nervous system by applying an in vitro blood-brain barrier and blood-cerebrospinal fluid (CSF) barrier based on monolayers of porcine brain microvessel endothelial cells (PMEC) or porcine choroid plexus epithelial cells (PCEC). Permeation studies through PMEC- and PCEC-monolayers were conducted for 60 min at drug concentrations of 1, 5, 10, and 30 muM applied to the donor compartment. PMEC were almost impermeable for AMS (permeation coefficient, P<1 x 10(-7) cm/s) in the resorptive direction, whereas transport in the secretory direction was observed with a P (+/-SD) of 5.2+/-3.6 x 10(-6) cm/s. The resorptive P of CLZ and DCLZ were 2.3+/-1.2 x 10(-4) and 9.6+/-5.0 x 10(-5) cm/s, respectively. For the permeation across PCEC in the resorptive direction, a P of 1.7+/-2.5 x 10(-6) cm/s was found for AMS and a P of 1.6+/-0.9 x 10(-4) and 2.3+/-1.3 x 10(-5) cm/s was calculated for CLZ and DCLZ, respectively. Both, CLZ and DCLZ, could easily pass both barriers with about a five-fold higher permeation rate of CLZ at the PCEC. The permeation of AMS across the BBB was restricted partly due to an efflux transport. It is thus suggested that AMS reaches its target structures via transport across the blood-CSF barrier.

Topics: Amisulpride; Animals; Antipsychotic Agents; Benzamides; Brain; Caco-2 Cells; Clozapine; Dose-Response Relationship, Drug; Humans; Sulpiride; Swine

2003