Neurological Disease

PF-05150122 is a novel potent and selective human Nav1.7 channel blocker with the activity of inhibiting human pain signaling. PF-05150122 exhibited favorable biopharmacokinetic parameters in microdose studies, providing a basis for exploring its application in acute or chronic pain inhibition. The pharmacokinetic model of PF-05150122 predicted that at the corresponding oral dose, it could effectively reduce the 50% inhibitory concentration (IC50) of Nav1.7, demonstrating its inhibitory potential.

TUG-2099 (compound 4s) is a potent GPR84 agonist with the EC₅₀ of 0.3 nM. TUG-2099 can be used for study of Alzheimer’s disease, atherosclerosis, cancer, and so an.

3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) is a potent dopamine uptake inhibitor. 3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) acts as a potent long-acting antihistaminic agent.

MBP Ac1-9 (4Y) is a synthetic peptide derived from a fragment of myelin basic protein (MBP) that has undergone specific chemical modifications. MBP Ac1-9 (4Y) is able to form a complex with the MHC class II molecule I-Au and activate specific T cell receptor (TCR), thus playing a role in the pathogenesis of experimental autoimmune encephalomyelitis (EAE). MBP Ac1-9 (4Y) can be used to study autoimmune diseases, especially those involving the central nervous system, such as multiple sclerosis.

BuChE-IN-10 (compound 7p) is an inhibitor of BuChE (eqBuChE IC₅₀ = 4.68 nM, huBuChE IC₅₀ = 9.12 nM). BuChE-IN-10 has anti-neuroinflammatory activity and exhibits high BBB permeability.

Paramethasone is an orally active long-acting glucocorticoid. Paramethasone directly inhibits testicular aromatase, thereby reducing the synthesis of estradiol. Paramethasone suppresses the basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone also decreases circulating levels of dihydrotestosterone, androstenedione and estradiol in male animals. Paramethasone inhibits cartilage degeneration and alleviates joint pathological damage in osteoarthritis models. Paramethasone can be used in research related to osteoarthritis and endocrinology.

Glaucine hydrobromide (O,O-Dimethylisoboldine hydrobromide; S-(+)-Glaucine hydrobromide; NSC 34396 hydrobromide) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine hydrobromide acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a K_i of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine hydrobromide induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine hydrobromide inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine hydrobromide holds potential for research in asthma and breast cancer.

C14TKL-1 is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).

Texas Red (Sulforhodamine 101) (solution) is an amphoteric rhodamine red fluorescent dye (excitation/emission: 586/605 nm). Texas Red is used extensively for investigating neuronal morphology and acts as acell type-selective fluorescent marker of astrocytes bothin vivoand in slice preparations.
Solvent and concentration: DMSO: 10 mM
The 1 mL volume is defined as the base specification. All larger sizes correspond to incremental volumes of this base.

PRL-8-53 is an orally active, blood-brain barrier-permeable benzoate derivative with potent spasmolytic activity and central nervous system regulatory activity. PRL-8-53 acts on dopamine, serotonin and cholinergic-related targets, enhances dopamine activity, partially inhibits serotonin function and elicits cholinergic responses, thereby maintaining neurotransmitter balance in the central nervous system. PRL-8-53 improves learning ability, short-term memory and long-term memory in animals. PRL-8-53 can be used in central nervous system-related research.

(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC₅₀ values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.

Necopidem (Compound 6) is a GABA A receptor modulator. Necopidem can be used in research on neurological disorders such as anxiety.

4-Ethyl pentedrone (p-Ethyl-α-methylamino-valerophenone) hydrochloride is a drug derivative.

(±)-Levomepromazine-d₄ ((±)-Methotrimeprazine-d₄) is the deuterium labeled (±)-Levomepromazine (HY-19489). (±)-Levomepromazine ((±)-Methotrimeprazine) is the racemate of Levomepromazine (HY-B1693).

Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of ³H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist.

Tyrosine 3-monooxygenase (Tyrosine hydroxylase) is a rate-limiting enzyme in catecholamine biosynthesis and belongs to the family of aromatic amino acid hydroxylases. Tyrosine 3-monooxygenase catalyzes the initial and rate-limiting step in the biosynthetic pathway of catecholamines, including dopamine, noradrenaline, and adrenaline.

1-(Pyridin-4-yl)heptan-1-one (Compound R=n-C₆H₁₃) is an anticonvulsant agent. 1-(Pyridin-4-yl)heptan-1-one can protect mice from electroshock-induced convulsions. 1-(Pyridin-4-yl)heptan-1-one is promising for research of convulsion-related diseases such as epilepsy.

3,4-Dichloro-α-pyrrolidinoisohexanophenone (3,4-Dichloro-α-PiHP) hydrochloride is an analogue of a psychoactive substance.

(S)-CPW 399 is a subtype-selective full agonist of AMPA receptors, with a 20-fold higher selectivity for GluA1 and GluA2 subunits over GluA3 and GluA4 subunits. (S)-CPW 399 can significantly increase the spontaneous firing rate (FR) of LC noradrenergic neurons by activating AMPA receptors containing GluA1 subunits. (S)-CPW 399 can be used for the study of neurological diseases.

Xestospongins and araguspongins are marine natural products first isolated from Pacific basin sponges, and noted to have vasodilatory properties.1 Inositol phosphates (IP) are important signal transduction messengers acting via IP3 receptors to promote the mobilization of Ca2+ from intracellular stores.2 Araguspongin B antagonizes the calcium-releasing action of inositol 1,4,5-trisphosphate at the receptor level in cerebral microsomes, with an IC₅₀ of 0.6 μM. It is nearly as potent as xestospongin C as an antagonist of the IP3 receptor.