clozapine

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Clozapine Analogues can be used to study neurological disorders.

N-Desmethyl clozapine-d8 Hydrochloride is a deuterated compound of N-Desmethyl clozapine Hydrochloride. N-Desmethyl clozapine Hydrochloride has a CAS number of 1189888-77-4.

Clozapine HCl is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.

Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. It targets ERα for degradation through the ubiquitin-proteasome system by utilizing the E3 ubiquitin ligase component N-recognin 5. This compound is applicable in cancer research. (Pink: ERα inhibitor; Black: linker; Blue: CRBN Ligand)

Clozapine N-oxide dihydrochloride, a derivative of Clozapine and an agonist of human muscarinic design receptors (DREADDs), crosses the blood-brain barrier and activates DREADD receptors hM3Dq and hM4Di.

Clozapine-d3 is a deuterated compound of Clozapine. Clozapine has a CAS number of 5786-21-0. Clozapine is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

N-Desmethyl clozapine-d8 is a deuterated compound of N-Desmethyl clozapine.

Clozapine-d8 is a deuterated compound of Clozapine.

Clozapine (HF 1854) dihydrochloride is utilized for researching psychiatric disorders. This compound exhibits high affinity for numerous neuroreceptors and acts as an effective antagonist of dopamine receptors, with a Ki value of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor, with Ki values of 9.5 nM and 4 nM, respectively. Additionally, Clozapine is a selective agonist of the muscarinic M4 receptor (EC50 = 11 nM).

N-Desmethylclozapine (Desmethylclozapine) is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist that binds to DREADD receptor subtypes [hM3Dq] and [hM4Di] with Ki values of 6.3 nM and 4.2 nM, respectively.

JHU37152 (JHU 37152) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

Belaperidone is an antipsychotic drug. It has a clozapine-like receptor profile and affinities for dopamine D(4) and 5-hydroxytryptamine(2A) receptors. LU111995 prolongs the Q-T interval to a limited degree and is not arrhythmogenic over the physiological

E3 LigaseLigand-linker Conjugate 161 is an E3 ubiquitin ligase ligand-linker conjugate (E3ligaseligand-linker conjugate) used in the synthesis of Tamoxifen-PEG-Clozapine.

OH-PEG3-C2-Succinamic acid-2-(Methylamino)ethanol serves as a PROTAC linker and is utilized in the synthesis of PROTAC Tamoxifen-PEG-Clozapine.

Olanzapine HCl is an atypical antipsychotic. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia and bipolar disorder. Olanzapine is structurally similar to clozapine and quetiapine. It is a dopamine antagonist and is classified as a thienobenzodiazepine.

JHU37160 (JHU 37160) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.