Neurological Disease

CDK17 is highly expressed in terminally differentiated neurons, particularly those found in hippocampal regions and olfactory bulbs. CDK17/p35NCK Recombinant Human Active Protein Kinase is an ortholog of CDK17.

Aβ/tau aggregation-IN-4 (Compound D21) is an Aβ/tau aggregation inhibitor. Aβ/tau aggregation-IN-4 promotes the degradation of Aβ40/42 (Aβ40, IC₅₀ = 2.151 μM; Aβ42, IC₅₀ = 3.622 μM). Aβ/tau aggregation-IN-4 shows selective AChE inhibition (IC₅₀: 5.56 μM). Aβ/tau aggregation-IN-4 inhibits MAO-A and MAO-B with IC₅₀s of 0.59 μM and 0.09 μM, respectively. Aβ/tau aggregation-IN-4 suppresses intracellular ROS levels. Aβ/tau aggregation-IN-4 can be used in the research of Alzheimer's disease.

FPR2 agonist 5 is a selective Formyl Peptide Receptor 2 (FPR2) agonist. FPR2 agonist 5 induces Ca²⁺ mobilization in FPR2-HL60 transfected cells with an EC₅₀ of 1.2 μM and causes FPR2 desensitization with an IC₅₀ of 0.32 μM. FPR2 agonist 5 exerts neuroprotective effects by mitigating LDH release, NO production, IL-1β, IL-6, IL-33, and IL-10 levels in LPS (HY-D1056)-induced mouse primary microglial cells. FPR2 agonist 5 can be used for the study of neuroinflammatory-related diseases.

Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [³H]CMD (IC₅₀ = 20 nM), than [³H]QNB, (IC₅₀ = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease.

EG01449 is a quinoline-based antagonist of Neuropilin-1 (NRP1) with an K_d of 0.6 µM. EG01449 competitively inhibits the binding of VEGFA to NRP1 with an IC₅₀ of 362 nM. EG01449 prevents VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 can be used for the research of nociceptive pain.

YM-796 dihydroxybutanedioate is a selective muscarinic M₁ receptor agonist. YM-796 dihydroxybutanedioate can improve cognitive impairment and reduce amyloid plaque deposition. YM-796 dihydroxybutanedioate can be used in the research of cognitive impairment diseases such as Alzheimer's disease.

DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a K_i of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects.

Propiomazine maleate is an orally active antihistamine agent. Propiomazine maleate is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine maleate is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.

α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC₅₀ value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity.

Juncusol, a phenanthrenoid found in Juncus setchuenensis, possesses anxiolytic effect. Juncusol is associated with metabolic changes in cortical serotonin/dopamine levels in Mice.

5-Methoxy-N,N-diethylpentylone (hydrochloride) is a drug analogue and can be used for the research of neurological disease.

OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a K_i of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC₅₀ of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (K_i=4.9 μM).

5-HT3 antagonist-7 (Compound 7e) is a competitive and selective 5-HT₃ receptor antagonist. 5-HT3 antagonist-7 inhibits 5-HT-induced contractions in guinea pig ileum and guinea pig thoracic aorta. 5-HT3 antagonist-7 prevents 2-methyl-5-HT-induced vomiting episodes in ferrets.

Fentrazamide (YRC 2388) is a herbicide. Fentrazamide has specific toxic effects on the nervous system and erythrocytes in rats, affecting the energy supply of cells mainly by interfering with the glycolysis process. Fentrazamide can be used as a useful tool to study the mechanisms of neurodegenerative diseases and erythrocyte dysfunction.

BMS-181885 is a selective 5-HT₁ receptor agonist and a ligand for 5-HT_1B/_1D receptors. BMS-181885 exhibits anti-migraine activity. BMS-181885 can be used in the research of neurological diseases such as migraine.

Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (K_d=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (K_d=6.4 pM) and Kv1.1 (K_d=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.

Enecadin hydrochloride is a neuroprotective agent extracted from patent US 8623823 B2.

GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics.

VU6077967 is a selective cannabinoid receptor 2 (CB2) agonist with an EC₅₀ of 8.6 nM for rCB2. VU6077967 can be used for the research of neurological disease, suah as Alzheimer’s disease.

Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.