excitatory

IDRA-21 is a positive AMPA receptor modulator.

LDN-212320 (OSU-0212320) is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

Ro 67-7476 is a positive allosteric modulator of mGluR1, which can enhance the calcium release induced by glutamate in HEK293 cells expressing rat mGluR1a. The EC50 is 60.1 nM. It is a P-ERK1/2 agonist, and can activate ERK1/2 phosphorylation without the addition of exogenous glutamate (EC50 = 163.3 nM).

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) is a thiopyridazine derivative that has been found to increase EAAT2 protein levels in astrocytes.

Cardioexcitatory peptide 1, a potent neuropeptide derived from Achatina atria, exerts significant excitatory effects on cardiac function, additionally influencing the motility of muscular tissues and neural activities [1].

Dopamine hydrochloride (ASL279) is a natural catecholamine neurotransmitter that mainly acts on dopamine receptors (D1-5 receptors) (EC50=2.7 nM). Dopamine hydrochloride induces VEGFR2 endocytosis through D2 dopamine receptor and has pro-angiogenic activity.

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.

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

DL-TBOA is an inhibitor of excitatory amino acid transporter proteins, inhibiting excitatory amino acid transporter protein 1 (EAAT1), EAAT2, and EAAT3.

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

L-Glutamic acid is an excitatory amino acid neurotransmitter and a Glutamic acid receptor agonist, including metabolic glutamic acid receptor (mGluR), AMPA receptor, NMDA receptor and KA receptor. L-Glutamic acid has an excitatory effect on the process of DA release from dopaminergic nerve endings. L-Glutamic acid can be used in the research of neurological diseases. L-Glutamic acid acts on ionic and metabolic Glutamic acid receptors.

L-Cysteic acid monohydrate (3-Sulfo-L-alanine Monohydrate) is an oxidation product of L-cysteine that may be used as a competitive inhibitor of the bacterial aspartate: alanine antiporter (AspT) exchange of aspartate and in other aspartate biological systems. L-Cysteic acid monohydrate is used in monomeric surfactant development. L-Cysteic acid monohydrate may be used in studies of excitatory amino acids in the brain, such as those that bind to cysteine sulfinic acid receptors. It is a useful agonist at several rat metabotropic glutamate receptors (mGluRs).

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

(S)-3-AMino-2-Methylpropanoic acid-HCl is an amino acid derivative that can be an agonist of the excitatory neurotransmitter glutamate and affect the nervous system.

Calcineurin Autoinhibitory Peptide acetate is a selectivecalcineurin phosphatase inhibitor(IC50 ~ 10 μM). Calcineurin Autoinhibitory Peptide acetate can be used in the protection of neurons from excitatory neuronal death.

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

(RS)-AMPA ((±)-AMPA) is a glutamate analog and an agonist of the effective and selective excitatory neurotransmitter L-glutamic acid.