central nervous system

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.

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

Vadocaine (Vadocaina) is a novel analgesic compound for local anaesthesia and can be used to study the central nervous system and cardiovascular system.

(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.

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

Nardeterol HCl is a β-adrenergic receptor partial agonist used in the study of the central nervous system.CAS 13460-73-83-4

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

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.

Gedocarnil(ZK 113315) may be used to study diseases of the central nervous system.

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.

Quinupramine (LM 208) is an orally available classical tricyclic antidepressant compound with a strong affinity for muscarinic and 5-HT receptors.Quinupramine crosses the central nervous system and can be used in the study of neurologic disorders.

Liafensine(BMS-820836) is a novel and selective triple monoamine reuptake inhibitor with inhibitory effects on the reuptake of serotonin, norepinephrine, and dopamine for the study of major depressive disorder and central nervous system disorders.

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.

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

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.

AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A) that penetrates the blood-brain barrier. It inhibits S-adenosylmethionine (SAM) metabolizing enzymes and MAT2A for the treatment of cancer and for studying the role of SAM regulation in the central nervous system (CNS).

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

Firategrast (SB 683699) is an orally active and specific α4β1 α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

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.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.2 0.3 0.2 nM for EGFR (L858R) EGFR (wt) EGFR (exon 19Del).

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Oxcarbazepine (GP 47680) is an Anti-epileptic Agent. The physiologic effect of oxcarbazepine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Uridine triacetate (RG 2133 triacetate) (Tri-O-acetyl uridine), an orally active prodrug of uridine, is efficiently absorbed in the gut and swiftly deacetylated in the circulation to release free uridine. It is utilized in the research of 5-fluorouracil (5-FU) and capecitabine toxicity, particularly targeting early-onset cardiac or central nervous system (CNS) complications.