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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
13 Results for "
cognitive efficacy
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "cognitive efficacy" in MCE Product Catalog:
3
3 Cited Publications
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ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
2
2 Cited Publications
Synonyms: S44819; Egis-13529
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Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
Cat. No.: HY-171844
CAS No.: 1086377-48-1
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CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury .
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Neurological Disease Metabolic Disease Inflammation/Immunology
PF-03654746 Tosylate is a potent, selective and brain-penetrant histamine H3 receptor antagonist. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
Cat. No.: HY-179004
CAS No.: 2640753-22-4
Synonyms: VU6022856
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ONO-9517601 is a potent, orally active, selective and CNS
penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an
MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm.
ONO-9517601 can be used for research on neurological and cognitive
disorders .
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ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
Cat. No.: HY-P991536
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Cat. No.: HY-11045
CAS No.: 935840-31-6
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Research Areas:
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.
PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis .
PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
Cat. No.: HY-179005
CAS No.: 2640753-27-9
Synonyms: VU6024391
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ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .
Cat. No.: HY-165527
CAS No.: 200398-40-9
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S18327 is a multi-target antipsychotic agent. S18327 exerts its efficacy by acting on multiple neurotransmitter systems in the brain, and it has antagonistic effects on dopamine receptors (particularly the D2 receptor) and 5-hydroxytryptamine 2A receptors (5-HT2A receptor). S18327 can counteract excessive dopamine activity and hypo-function of glutamate. S18327 exhibits a multi-parameter pharmacological profile that is highly similar to that of Clozapine (HY-14539). S18327 can produce the same discriminative stimulus as Clozapine, improve cognitive filtering deficits associated with schizophrenia, and display anxiolytic properties. S18327 has relatively weak affinity for histaminergic receptors and muscarinic receptors, which avoids the side effects of Clozapine .
Cat. No.: HY-120783
CAS No.: 1531592-40-1
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Lu AF58801 is a potent, orally available, brain-penetrant positive allosteric modulator of α7 nicotinic acetylcholine receptors with efficacy in a novel object recognition task in mice. Lu AF58801 was shown to selectively enhance the activity of α7 nicotinic acetylcholine receptors. Lu AF58801 was able to improve cognitive function in mice treated with subchronic fluchlorothiazol (PCP) .
Cat. No.: HY-169156
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HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models .
Cat. No.: HY-12193
CAS No.: 556835-30-4
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A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
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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
