Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H19ClN4 |
| Molecular Weight | 326.823 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCN(CC1)C2=NC3=C(NC4=C2C=C(Cl)C=C4)C=CC=C3
InChI
InChIKey=APOMSSAGEAOUGO-UHFFFAOYSA-N
InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-12-13(19)6-7-15(14)20-16-4-2-3-5-17(16)21-18/h2-7,12,20H,8-11H2,1H3
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/10377229Curator's Comment: description was created based on several sources, including
http://pubs.acs.org/doi/abs/10.1021/jm9704457 | https://www.ncbi.nlm.nih.gov/pubmed/8101877 | https://www.ncbi.nlm.nih.gov/pubmed/11561066 | https://www.ncbi.nlm.nih.gov/pubmed/9723970
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377229
Curator's Comment: description was created based on several sources, including
http://pubs.acs.org/doi/abs/10.1021/jm9704457 | https://www.ncbi.nlm.nih.gov/pubmed/8101877 | https://www.ncbi.nlm.nih.gov/pubmed/11561066 | https://www.ncbi.nlm.nih.gov/pubmed/9723970
ISOCLOZAPINE is typical antipsychotic that acts by blocking the receptors in the brain’s dopamine pathways. Isoclozapine
has high affinities at both DA (D1 and D2) and serotonin (5-HT2A and 5-HT2C) receptors. Isoclozapine shows the greatest antipsychotic potential on inhibition of apomorphine-induced climbing in mice at quite low doses under sc or po administrations. However, Isoclozapine also produces catalepsy at low doses.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL265 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8101877 |
28.0 nM [Ki] | ||
Target ID: CHEMBL324 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377229 |
2.9 nM [IC50] | ||
Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377229 |
12.0 nM [IC50] | ||
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377229 |
34.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9406603
Male rats of a Wistar-derived strain (Harlan, Zeist, The Netherlands) weighing 175-225 g were used. ISOCLOZAPINE (0.3, 1, 3, 10, 30 mkM/kg) were administered Subcutaneously 30 min before the administration of 1 mg/kg apomorphine. After administration of apomorphine, rats were transferred to an automated activity monitoring system (Automex II, Columbus, OH) and activity was measured for 30 min. Experiments were done in parallel on four different animals and per session three experimental groups and one salinetreated group were studied.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377229
Incubations were carried out in 50 mM Tris-HCl buffer, pH 7.35, containing 120 mM NaCl, 5 mM MgCl2, and 1 mM EDTA. The assay contained in a total volume of 1 mL: 0.15 nM [3H]spiperone, specific radioactivity 3.6 TBq/mmol, and membranes of A9L cells expressing the human D2 dopamine receptor (40-60 íg of protein/assay). Incubations were run for 15 min at 37 °C and terminated by rapid filtration on Whatman GF/B filters and 3 washes with ice-cold 50 mM Tris-HCl buffer, pH 7.35 (without salts and EDTA). Nonspecific binding was determined in the presence of 1 mM (+)-butaclamol.
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