cns disorders

Budipine is a low affinity, N-methyl-D-aspartate receptor antagonist,is an antiparkinsonian agent.

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

AVN-322 is an orally active and specific 5-HT6R antagonist for the study of CNS disorders such as impaired memory and schizophrenia.

BW-1370U87 is a reversible competitive monoamine oxidase-A inhibitor for the study of depression and other CNS disorders.

JNJ-26489112 is a CNS-active agent and inhibitor of voltage-gated Na+ channels and N-type Ca2+ channels with broad-spectrum anticonvulsant activity in rodents and can be used to study neurological disorders.

N-(3-Methoxybenzyl)Palmitamide is a promising FAAH inhibitor for the treatment of pain, inflammation, and CNS degenerative disorders.

PDE10-IN-1 (SEP-0372814) is used for treating CNS and metabolic disorders.

Neurotensin TFA (39379-15-2 free base) is an endogenous 13 amino acid neuropeptide with profound opioid-independent analgesic effects. It behaves as a neurotransmitter in the brain, as a hormone in the gut, and also as a neuromodulator. It is implicated in the pathophysiology of several CNS disorders (including schizophrenia, Parkinson's disease, drug abuse, pain, cancer, inflammation, eating disorders, and central control of blood pressure) due to its association with a wide variety of neurotransmitter systems such as dopaminergic, sertonergic, glutamatergic, GABAergic, and cholinergic systems. It has a role as a human metabolite, a mitogen, a neurotransmitter and a vulnerary.

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

N-Ethyl-N-nitrosourea (ENU) is a DNA alkylating agent. It induces leukemia by alkylating nucleobases, thereby damaging DNA, which leads to bone marrow suppression and the development of leukemia cells. ENU is teratogenic in vivo, causing tumor formation and foot malformations in pregnant rats. Additionally, it can result in central nervous system (CNS) tumors and genetic disorders.

ONO-2920632 is an orally active and CNS-penetrant TREK channel activator with EC50 values of 0.3 µM for TREK-1 and 2.8 µM for TREK-2. It demonstrates selectivity for other K2P channels, showing over 91-fold selectivity against TASK1, TASK2, TASK3, TRAAK, TWIK2, and 31-fold selectivity against TRESK. ONO-2920632 exhibits analgesic effects and is used in the study of pain, migraine, and neurological disorders.

α5-GABAA receptor modulator 1 (Compound A-4) is a selective silent allosteric modulator (SAM) targeting the α5 subunit of GABAA receptors, useful for research into central nervous system (CNS) disorders.

KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.

Deanol acetamidobenzoate is CNS stimulant. It can be caused elevated blood choline levels, can be used in Treatment of Choreiform Movement Disorders.

Ganglioside GM2 is a glycosphingolipid component of cellular membranes, primarily the plasma membrane. Levels of ganglioside GM2 are elevated in the brain of patients with Sandhoff disease, as well as feline and mouse models of the disease. Ganglioside GM2 accumulates in the lysosomes of individuals with Tay-Sachs disease and GM2-activator deficiency, as well as in the CNS of patients with and animal models of mucopolysaccharide storage disorders and Niemann-Pick disease types A, C1, and C2. Ganglioside GM2 mixture contains ganglioside GM2 molecular species with C18:1 and C20:1 sphingoid backbones.

Certain chronic neurologic disorders, such as Parkinson's disease, are caused by an insufficiency of the neurotransmitter dopamine secondary to the degeneration of substantia nigra dopaminergic neurons. N-(α-Linolenoyl) tyrosine (NALT) is a simple α-amide conjugate between the ω-3 essential fatty acid α-linolenate and the amino acid tyrosine. α-Linolenate is an important precursor to docosahexaenoic acid (DHA), a prominent brain polyunsaturated fatty acid, while tyrosine is the metabolic precursor for neuronal dopamine synthesis. NALT was prepared as a method for enhancing central nervous system (CNS) dopamine content by facilitated transport of the tyrosine precursor across the blood-brain barrier. In experimental rat models of dopamine insufficiency, NALT increased CNS dopamine levels and exhibited an activity profile consistent with an anti-Parkinson's therapeutic agent.

N-Benzylpalmitamide (Macamide 1) inhibits fatty acid amide hydrolase (FAAH) in a time-dependent manner and could potentially offer a good alternative for the treatment of pain, inflammation and CNS degenerative disorders.

R-PSOP is a potent and selective nonpeptidic NMUR2 antagonist, exhibiting binding affinity to human and rat NMUR2 with Ki values of 52 nM and 32 nM, respectively. This compound demonstrates moderate central nervous system (CNS) penetration and is valuable in the study of eating disorders, obesity, pain, and stress-related disorders [1].

5-HT7 agonist 2 is a highly potent 5-HT7 receptor agonist with an IC50 value of 28.7 nM, and it holds promise for studying and understanding various Central Nervous System (CNS) disorders [1].

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective compound (Ki=2.16 nM) that exhibits potential therapeutic effects in CNS disorders.

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.

NYX-2925, an orally active NMDAR (N-methyl-D-aspartate receptor) modulator, enhances activated Src levels and Src phosphorylation at GluN2A and GluN2B sites in the mPFC (medial prefrontal cortex), without affecting CAMKII (Ca2+ calmodulin-dependent protein kinase II) or exhibiting addictive or sedative ataxic side effects. It is utilized in the study of various CNS (central nervous system) disorders mediated by NMDA receptors.

SXC 2023 ((S)-2-acetamido-3-(4-methylbenzoylthio)propanoic acid) is a therapeutic prodrug of N-acetyl-L-cysteine for the treatment of CNS disorders and neurocognitive disorders, and can be used to treat glutamatergic dysfunction and psychiatric disorders in which oxidative stress plays a key role.

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. The free base form of this compound is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, PTSD, seizure disorders, and additional CNS disorders [1].