nervous system

Emamectin Benzoate (MK-244), by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as a chloride channel activator.

Antazoline has antihistamine and anticholinergic effects.It used to treat a variety of arrhythmias.

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

γ-Aminobutyric acid belongs to natural products and functions as an agonist of GABAA and GABAB receptors, possessing central sedative effects, cell permeability, and the ability to modulate neuronal excitability. This compound is used in neuroscience research and exhibits anxiolytic, anticonvulsant, and neuroprotective activities.

Gadoteridol (Gd-HP-DO3A) is a gadolinium-based MRI contrast agent that can be used for central nervous system imaging.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

Apelin-13 is a 13-amino acid peptide sequence found in the central and peripheral nervous system that is an endogenous ligand for the G protein-coupled receptor angiotensin II protein J (APJ), with an EC50 value of 0.37 nM for APJ.Apelin-13 has vasodilatory and antihypertensive activity and can be used to study type 2 diabetic syndrome. Apelin-13 has vasodilatory and antihypertensive activities and can be used to study type 2 diabetes syndrome.

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

Pentiapine (CGS 10746) is a small-molecule inhibitor and a dopamine release inhibitor with cell permeability, used in neuropharmacological research to modulate dopaminergic signaling, holding significant application value in studies related to nervous system mechanisms.

Kainic acid is an excitatory amino acid receptor agonist (EC50=16.2 μM). Kainic acid is an effective excitatory toxic agent. Kainic acid induces epileptic seizures.

Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.

Angiotensin II is a major biologically active vasoconstrictor peptide that regulates blood pressure by binding to AT1R and AT2R receptors. It stimulates the sympathetic nervous system, promotes aldosterone synthesis, and enhances renal function. Additionally, it induces vascular smooth muscle cell proliferation and increases collagen synthesis, leading to vascular and myocardial hypertrophy and fibrosis. It also promotes apoptosis and endothelial capillary formation. Angiotensin II is commonly used to induce hypertension and cardiac hypertrophy animal models.

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

Antipsychotic agent 54 is a benzoylpiperidine compound that can be used in the study of central nervous system diseases such as psychosis and cognitive impairment.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

Besipirdine hydrochloride is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine hydrochloride inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine hydrochloride reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system in rats.

JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.

Landipirdine (RO-5025181) is a selective 5-HT6R antagonist for the study of central nervous system disorders such as dementia.

(R)-PF-04822163 is an isomer of PF-04822163. PF-04822163 is an oral, selective PDE1 inhibitor that can cross the blood-brain barrier. PF-04822163 can be used in studies about nervous system disorders such as attention deficit hyperactivity disorder (ADHD) and Parkinson’s disease.

Cafedrine (Cafedrin) is found in tea and coffee and has a central nervous system stimulant effect.Cafedrine is often used in a 20:1 combination with a fixed dose of cortisone in the study of acute hypotension.