gad-α

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Hydroxyzine (Hydroxyzine free base) is an antagonist of histamine H1-receptor.

BNC210 (IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol/g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol/kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg/0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

GAD65 (206-220) is a synthetic peptide derived from glutamic acid decarboxylase (GAD) 65, specifically corresponding to residues 180-188. It is known that GAD65 interacts with I-Ag7 MHC class II molecules and is a significant pancreatic antigen that self-reactive T cells target in type I diabetes mellitus.

Gadopentetic acid (gadolinium complex) (Gd-DTPA) is an paramagnetic contrast agent commonly implemented by a bolus intravenous injection (i.v.) in Dynamic contrast-enhanced MRI (DCE-MRI) studies.

Tegadifur (40497S) is an orally available antitumor compound with antimetabolic effects, often used with uracil and in the treatment of rectal adenocarcinoma.

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.

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

Gadolinium chloride is a calcium-sensing receptor (CaSR) agonist

Gadopentetate dimeglumine is used in magnetic resonance imaging (MRI) to allow blood vessels, organs and other non-bone tissues to be visualized more clearly.Gadopentetate dimeglumine induces atrophy of spermatogonia.

(-)-Verbenone is a naturally occurring terpene found in the leaves of Suregada zanzibariensis Verdc.Verbenone has anti-aggregation pheromone effects and interrupts the attraction of bark beetles to its aggregation pheromone.

Chelidamic acid is a heterocyclic organic acid with a pyran skeleton and acts as an inhibitor of glutamate decarboxylase, with a Ki of 33 μM.

Gadolinium(III) chloride hexahydrate is a contrast agent in magnetic resonance imaging and can be used in medicine, magnetic resonance imaging, liquid crystal displays and other fields. Gadolinium(III) chloride hexahydrate can be used to synthesize complexes and nanomaterials.

Regadenoson is an A2A adenosine receptor agonist, a coronary vasodilator commonly used in pharmacologic stress testing.

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

Timegadine is a competitive inhibitor of COX and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates and in washed rabbit platelets.

Gadoxetate Disodium is used to evaluate focal liver lesions, such as hepatocellular carcinoma or liver metastasis on T1-weighted imaging. It is a contrast agent in magnetic resonance imaging (MRI) of the hepatobiliary system. It accumulates in normal, fun

Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

Timegadine hydrochloride (SR1368 hydrochloride) is the hydrochloride salt form of Timegadine. It is an orally active inhibitor of COX and lipo-oxygenase, effectively suppressing COX in rabbit platelets and rat brain with IC50 values of 5 nM and 20 μM, respectively, and inhibiting lipo-oxygenase in horse and rabbit platelets with an IC50 of 100 μM. Timegadine hydrochloride also exhibits anti-arthritis activity.

DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.