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Aromatic organic heterocyclic compounds that consist of benzene fused with a diazepine ring; diazepine rings are seven-membered heterocyclic compounds with two nitrogen atoms.
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Clozapine N-oxide is a major metabolite of clozapine and a human muscarinic designer receptors (DREADDs) agonist. It activates the DREADD receptor hM3Dq and hM4Di but cannot cross the blood-brain barrier. Its parent compound, clozapine, is a potent dopamine antagonist and a potent and selective muscarinic M4 receptor agonist. For research use only.
DREADD activator
Metabolite of clozapine
Activates hM3Dq and hM4Di DREADD receptors
Cannot cross the blood-brain barrier
Solid appearance, light yellow to yellow color
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Also available in 5 mg, 10 mg, 25 mg, 50 mg, 100 mg and bulk. Please contact Fisher for quotes. Clozapine Analogues can be used to study neurological disorders. Purity 99.6%
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Clozapine N-oxide (CNO CAS 34233-69-7) is a metabolic derivative of the atypical antipsychotic drug clozapine primarily known for its applications as a chemogenetic actuator Biologically inert in typical mammalian systems CNO selectively activates engineered muscarinic receptors such as the M3-designer receptors exclusively activated by designer drugs (DREADDs) Additionally CNO influences receptor expression levels exposure in cortical neuron cultures reduces 5-HT2 receptor density significantly Due to its specificity CNO is extensively utilized in neuroscience research to modulate neuronal activity non-invasively through chemogenetic approaches
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Clozapine (CAS 5786-21-0) is an atypical antipsychotic agent extensively studied for treating schizophrenia refractory to standard antipsychotics Clozapine exhibits high affinity binding to serotonin receptors 5-HT1c and 5-HT2 with reported pKi values of 8 07 and 7 63 respectively Additionally clozapine interacts with multiple dopamine receptor subtypes (D1-D5) displaying Ki values of 141 nM (D1) 80 nM (D2) 230 nM (D3) 89 nM (D4) and 250 nM (D5) Due to its distinctive receptor affinity profile clozapine serves as an important pharmacological tool in research on serotonin- and dopamine-mediated signaling mechanisms in psychiatric disorders
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Coelenterazine (CAS 55779-48-1) is a small molecule substrate for bioluminescent enzymes that generates a chemiluminescent signal upon oxidation by reactive oxygen species (ROS) particularly superoxide anions and peroxynitrite In rat hepatocytes it exhibits an IC50 of approximately 69 M toward superoxide anions Coelenterazine demonstrates concentration-dependent antioxidant activity enhancing cell viability and decreasing lipid peroxidation under oxidative stress induced by tert-butyl hydroperoxide It is widely applied in biomedical research including ELISA bioluminescence resonance energy transfer (BRET) high-throughput screening (HTS) and in vivo imaging studies of ROS in cancer models
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Clozapine is an antipsychotic used for the research of schizophrenia. It has high affinity for several neuroreceptors. Clozapine acts as a potent antagonist of dopamine D2 with a Ki of 75 nM. It also inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Ki values of 9.5 nM and 4 nM, respectively. Furthermore, Clozapine is a potent and selective agonist at the muscarinic M4 receptor (EC50 = 11 nM).
Antagonist of dopamine D2 and α2-adrenoceptor
Inhibits muscarinic M1 and serotonin 5HT2A receptors
Potent and selective agonist at muscarinic M4 receptor
Exhibits antipsychotic effects in mouse models
Inhibits human dopamine receptor D4.2 and D2L receptor
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Coelenterazine is a luminescent enzyme substrate for apoaequorin and Renilla luciferase. It has been used as a bioluminescence donor in bioluminescence resonance energy transfer (BRET) to detect protein-protein interactions. It is also a superoxide anion-sensitive chemiluminescent probe that can be used in the chemiluminescent detection of peroxynitrite (Ex/Em = 429/466 nm).
Luminescent enzyme substrate for apoaequorin and Renilla luciferase.
Used in bioluminescence resonance energy transfer (BRET) to detect protein-protein interactions.