excitation

Optovin is a TRPA1 activator, which is reversibly photoactivated.

Meclinertant (SR 48692) is a neurotensin receptor-1 (NT1) antagonist that blocks neurotensin-induced excitation and can be used to study neurological disorders.

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Dantrolene sodium (Dantrolene sodium salt) is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Dantrolene sodium hemiheptahydrate (Sodium dantrolene) is the sodium salt form of dantrolene, a hydantoin derivative, and direct-acting skeletal muscle relaxant.

Photosensitizer-3, a photosensitizer that generates single-linear oxygen upon near-infrared light excitation in combination with FAP, exhibited potent and selective killing of transfected HEK cells and affibody-targeted A431 cancer cells.

Ac-LETD-AFC is a fluorescent substrate specifically cleaved by caspase-8 and can be used to quantify caspase activity by fluorescence detection of free AFC.Ac-LETD-AFC has an excitation wavelength of 400 nm and an emission wavelength of 505 nm.

Filipin III is extracted from strain KPE18H and has significant antifungal activity.

TAMRA-PEG3-Azide is a TAMRA red fluorescent dye linker with a maximum excitation emission wavelength of 553 575 nm.

resorufin galactopyranoside is a fluorescent substrate for β-galactosidase.After cleavage by β-galactosidase, the fluorescent portion of resorufin is released and its fluorescence can be used to quantify β-galactosidase activity. It has an excitation light of 570 and an emission light of 580 nm.

CY5-SE Ditriethylamine salt is a reactive dye for the labeling of amino-groups in peptides, proteins, and oligonucleotides. Excitation (nm):649, Emission (nm): 670.

EC-17 (disodium salt), a folate receptor alpha (FRα) targeting contrast agent, exhibits fluorescent properties within the visible light spectrum, characterized by peak excitation and emission wavelengths of 470/520 nm, respectively.

(S)-Baclofen has effects on excitation in the ascending auditory pathway leading to it a potential reagent for the treatment of hyperactive auditory disorders such as hyperacusis and tinnitus.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

FFN 511 hydrochloride is a fluorescent pseudo-neurotransmitters (FFNs) targeting neuronal vesicular monoamine transporter 2 (VMA T2).FFN 511 hydrochloride inhibits the binding of 5-hydroxytryptamine to VMA T2-containing membranes and can be used for labelling of dopaminergic nerve endings in acute slices of in vivo cortex-striatum. The excitation and emission maxima are 406 and 501 nm, respectively.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

NIM-7 is a fluorescent probe, allowing lipid droplets and lysosomes to be labelled simultaneously and with high specificity, being visualized readily through yellow and red fluorescence, using different excitation and detection channels.

Ryanodol is a complex diterpenoid that modulates intracellular calcium-ion release at ryanodine receptors, ion channels critical for skeletal and cardiac muscle excitation-contraction coupling and synaptic transmission.

VU0456940 is a potent M1 PAM with excellent selectivity (hM1 EC50 = 340 nM, 14-fold leftward shift of the ACh CRC; hM2–hM5 inactive). VU0456940 potentiated the excitation of a subthreshold concentration of CCh in MSNs. VU0456940 shifted APP processing and

The renin fluorogenic substrate consists of the normal peptide substrate for renin which has been linked to the fluorophore EDANS at one end and to a non-fluorescent quenching molecule (Dabcyl) at the other. After cleavage by renin, the product (peptide-EDANS) is brightly fluorescent and can be easily analyzed using an excitation wavelength of 340 nm and emission wavelengths of 485-510 nm.

Gly-Arg-AMC is a fluorogenic substrate for cathepsin C.1 Upon enzymatic cleavage by cathepsin C, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify cathepsin C activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. |1. Rubach, J.K., Cui, G., Schneck, J.L., et al. The amino-acid substituents of dipeptide substrates of cathepsin C can determine the rate-limiting steps of catalysis. Biochemistry 51(38), 7551-7568 (2012).

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm

BODIPY-C12 Ceramide (B12Cer) is a fluorescently-tagged form of C12 ceramide, with excitation/emission maxima at 505/540 nm, respectively. It is a fluorescently-labeled sphingolipid and has been utilized for quantifying acid sphingomyelinase activity in the plasma of patients with Niemann-Pick disease.