Glycine-2-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
Phe-Met-Arg-Phe, amide dose dependently (ED50=23 nM) activates a K+ current in the peptidergic caudodorsal neurons.
(S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist[1][2].
Digoxin is a potent inhibitor of Na+/K+-ATPase, clinically used to treat arrhythmia and heart failure.
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo[1][2].
Globotriaosylsphingosine (lyso-Gb3) inhibits the growth of fibroblasts, as well as their differentiation into myofibroblasts, and collagen expression. Globotriaosylsphingosine can be used for Fabry disease research[1].
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety[1].
SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM[1].
Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways[1][2][4].
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus[1][2].
ROMK-IN-32 is a potent, selective ROMK inhibitor with IC50 of 17 nM; shows an improved functional hERG/ROMK potency ratio (1176x) and preclinical PK profile; demonstrates blood pressure lowering effects in the spontaneously hypertensive rat model.
Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens[1].
Aneratrigine is a sodium channel protein type 9 subunit alpha blocker. Aneratrigine can be used for neuropathic pain diseases research[1].
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease[1][2][3][4].
Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.
Dequalinium Chloride is a selective blocker of apamin-sensitive K+ channels.Target: Potassium ChannelDequalinium Chloride is a selective blocker of apamin-sensitive K+ channels. Treatment with Dequalinium chloride did not influence conditions caused by haemolytic streptococci -- verified by bacteriological examinations of pharyngeal smears -- inspite of its efficiency in vitro [1]. Dequalinium chloride (DECA), a cationic, lipophilic mitochondrial poison, selectively targets the mitochondrial membrane of certain epithelial carcinoma cells, in which it inhibits cellular energy production. Higher DECA doses under either regimen induced severe toxic effects and mortality [2].
Propafenone D7 hydrochloride is the deuterium labeled Propafenone, which is a classic anti-arrhythmic medication.
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research[1].
(-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent[1].
αA-Conotoxin OIVA (αA-OIVA) is a selective nAChR antagonist with an IC50 of 56 nM against mammalian fetal muscle nAChR. αA-Conotoxin OIVA is a peptide that can be derived from conotoxin. αA-Conotoxin OIVA paralyzes muscles[1][2].
PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM); increases action potential rheobase in small diameter mDRG neurons, demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca2+ channel blocker. ω-Agatoxin TK inhibits the high K+ depolarisation-induced rise in internal Ca2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels[1][2][3].
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors[1].
GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
Phenylpiracetam(Phenotropyl; Phenotropil) is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam.IC50 Value:Target: AMPA receptor allosteric modulatorin vitro: N/Ain vivo: In the open-field test, a significant increase in locomotor activity was observed after a single administration of R-phenotropil at doses of 10 and 50 mg/kg and S-phenotropil at a dose of 50 mg/kg. In the forced swim test, R-phenotropil induced an antidepressant effect at doses of 100 and 50 mg/kg, and S-phenotropil was active at a dose of 100 mg/kg. R-phenotropil significantly enhanced memory function in a passive avoidance response test at a dose of 1 mg/kg; the S-enantiomer did not show any activity in this test [1].
A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. IC50 value: Target: P2X2/3It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.
N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na+ channels[1].
NAV 26 (compound 26) is a selective voltage-gated sodium channel Nav1.7 blocker with an IC50 of 0.37 μM. NAV 26 can be used for pain research[1].