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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
D2L
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "D2L" in MCE Product Catalog:
6
6 Cited Publications
Synonyms: OPC-34712
Áreas de investigación:
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [2].
Target:
Áreas de investigación:
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder [2].
Target:
Áreas de investigación:
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons [2].
Synonyms: OPC-34712-d8-1
Referencia número: HY-133152
No. CAS: 1191900-51-2
Synonyms: DM-3411
Target:
Áreas de investigación:
Brexpiprazole S-oxide (DM-3411) is a metabolite of Brexpiprazole (HY-15780). Brexpiprazole S-oxide is a dopamine D2 receptor ligand that binds to the human dopamine D2L receptor with a Ki of 5.01 nM. Brexpiprazole S-oxide can be used for research on schizophrenia [2] .
Referencia número: HY-15780R
No. CAS: 913611-97-9
Synonyms: OPC-34712 (Standard)
Áreas de investigación:
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [2].
Synonyms: OPC-34712-d8
Referencia número: HY-A0077S1
No. CAS: 155593-75-2
Referencia número: HY-177122
No. CAS: 3034857-88-7
Target:
Áreas de investigación:
Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
Synonyms: DM-3411 d8
Áreas de investigación:
Brexpiprazole S-oxide-d8 (DM-3411 D8) is the deuterated-labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide (DM-3411) is a metabolite of Brexpiprazole (HY-15780). Brexpiprazole S-oxide is a dopamine D2 receptor ligand that binds to the human dopamine D2L receptor with a Ki of 5.01 nM. Brexpiprazole S-oxide can be used for research on schizophrenia [2] .
Referencia número: HY-15780A
No. CAS: 913612-38-1
Synonyms: OPC-34712 hydrochloride
Áreas de investigación:
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [2].
Referencia número: HY-112320
No. CAS: 14862-80-7
Target:
Áreas de investigación:
UCSF34 (Compound 54) is a Haloperidol (HY-14538) analogue. UCSF34 binds to the human D2L receptor, with an estimated pKi of 7.49. UCSF34 can be used in the research of schizophrenia .
Referencia número: HY-34763
No. CAS: 70500-72-0
Synonyms: 7-Hydroxyquinolinone; 2,7-Dihydroxyquinoline
Target:
Áreas de investigación:
7-Hydroxycarbostyril (7-Hydroxy-2(1H)-quinolinone) (Compound 7) is a quinolinone derivative. 7-Hydroxycarbostyril can be used for synthesis of Brexpiprazole (HY-15780). Brexpiprazole, a typical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor .
Referencia número: HY-119389
No. CAS: 207277-37-0
Target:
Áreas de investigación:
RGH-1756 is an atypical antipsychotic that has a strong and selective antagonist activity on human D3 and less pronounced activity on human D2L and 5HT1A receptors .
Referencia número: HY-111066AR
No. CAS: 2108806-02-4
Target:
Áreas de investigación:
JNJ-37822681 (dihydrochloride) (Standard) is the analytical standard of JNJ-37822681 (dihydrochloride). This product is intended for research and analytical applications. JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder [2].
Referencia número: HY-171328
No. CAS: 1076189-55-3
Target:
Áreas de investigación:
RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [ 35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity .
Referencia número: HY-111136
No. CAS: 916898-61-8
Áreas de investigación:
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
Referencia número: HY-100658S
No. CAS: 1308279-08-4
Referencia número: HY-100658R
No. CAS: 839712-25-3
Áreas de investigación:
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons [2].
Referencia número: HY-L165
282 compounds
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life.
MCE designs a unique collection of 282 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
