Deltorphin 2 is a selective peptide agonit for the δ opioid receptor.
Resorufin butyrate is a fluorogenic substrate for triglyceride lipases and cholinesterase (Ex=570 nm, Em=580 nm)[1][2][3].
Memantine, an amantadine derivative with low to moderate-affinity for NMDA receptors, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively..Target: NMDA Receptor, Memantine (Ebixa, Axura, Namenda, Akatinol) is a moderate-affinity, uncompetitive, voltage-dependent, NMDA-receptor antagonist with fast on/off kinetics that inhibits excessive calcium influx induced by chronic overstimulation of the NMDA receptor. Memantine is approved in the US and the EU for the treatment of patients with moderate to severe dementia of the Alzheimer's type [1]. Memantine has considerable therapeutic potential for the myriad of clinical entities associated with NMDA receptor-mediated neurotoxicity [2]. Memantine blocked 200 microM NMDA-evoked responses with a 50% inhibition constant (IC50) of approximately 1 microM at -60 mV and an empirical Hill coefficient of approximately 1 [3].
(RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors[1][2].
Deudextromethorphan (AVP-786) is a deuterated form of dextromethorphan/quinidine (AVP-923, Nuedexta). Deudextromethorphan, a glutamate-targeting agent, is an orally active N-methyl-D-aspartate (NMDA) receptor antagonist. Deudextromethorphan can be used for the research of Pseudo-Bulbar Affect, traumatic brain injury, behavioral disinhibition and agitation in AD[1][2][3].
MRK-623 is a potent, α2/α3 subunit functionally selectiviie GABAA receptor agonist.
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a selective agonist at GABAA receptors that contain α4-δ subunits, and has anxiolytic and sedative effects[1].
TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats.
Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.IC50 value:Target: 5-HT4 agonistin vitro: Prucalopride was a 5-HT(4) receptor agonist in the guinea-pig colon, as it induced contractions (pEC(50)=7.48+/-0.06; insensitive to a 5-HT(2A) or 5-HT(3) receptor antagonist, but inhibited by a 5-HT(4) receptor antagonist) as well as the facilitation of electrical stimulation-induced noncholinergic contractions (blocked by a 5-HT(4) receptor antagonist). Prucalopride did not cause relevant inhibition of 5-HT(2A), 5-HT(2B), or 5-HT(3), motilin or cholecystokinin (CCK(1)) receptor-mediated contractions, nor nicotinic or muscarinic acetylcholine receptor-mediated contractions, up to 10 microM [1].in vivo: Rat microdialysis studies revealed that prucalopride maximally increased ACh and histamine levels in the prefrontal cortex at 5 and 10 mg/kg, whereas PRX-03140 significantly increased cortical histamine levels at 50 mg/kg, failing to affect ACh release at doses lower than 150 mg/kg [2].
DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively)[1].
GYKI 52466 dihydrochloride is a potent, selective, orally active and non-competitive kainate- and AMPA-activated currents antagonist with IC50s of 7.5 μM and 11 μM, respectively. GYKI 52466 dihydrochloride is inactive against N-methyl-D-aspartate (NMDA) or γ-aminobutyric acid responses. GYKI 52466 dihydrochloride ia a muscle relaxant and anticonvulsant agent, and has good blood brain barrier permeability[1][2].
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease[1].
Pralidoxime chloride is a useful agent in the treatment of organophosphate poisoning. Pralidoxime binds to organophosphate-inactivated acetylcholinesterase, used to combat poisoning by organophosphates or acetylcholinesterase inhibitors (nerve agents) in conjunction with atropine and diazepam.
Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism[1].
UCSF648 (Compound 5A6-48) is a chemical probe for the 5-HT5A serotonin receptor. UCSF648 weakly activates ADRA2A and MTNR1A[1].
Ondansetron(GR38032) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.IC50 Value: Target: 5- HT3 Receptorin vitro: 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) [1]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response [2].in vivo: Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating [3]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg [4]. ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection [5]. Toxicity: Ondansetron may be safe in lower doses used to prevent nausea and vomiting in radiation treatment or postoperatively. However, as there is a report that a lower dose of ondansetron prolonged the QT interval in healthy volunteers, this needs to be clarified by the FDA [6].
Substance P-Gly-Lys-Arg, also known as β-Preprotachykinin (58-71), is an analog of Substance P (Substance P (HY-P0201))[1].
β-CGRP, human is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.
Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a Ki of 0.010 mM.
Pargyline is an irreversible non-selective monoamine oxidase (MAO) inhibitor drug (IC50 for MAO-A is 11.52 nM and for MAO-B is 8.2 nM) .
MM 77 dihydrochloride is a potent postsynaptic antagonist of the 5-HT1A receptor. MM 77 dihydrochloride exhibits anxiolytic-like activity[1][2].
L-Glutamic acid-13C5,15N is the 13C- and 15N-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Herkinorin is a potent and selective agonist of µ opioid receptor with a Ki of 45 nM Herkinorin is widely used for pain research[1].
Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist[1]. Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects[2].
Mesembrine-d3 ((+)-Mesembrine-d3) is the deuterium labeled Mesembrine. Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM[1][2].
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research[1][2].
(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.IC50 value: 44.8 uM(EC50) [1]Target: AMPA/kainate receptor agonistin vitro: The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses [1]. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50% [2].in vivo: In newborn mice (P5, histopathology at P10), local injection of the AMPA receptor agonist S-bromo-willardiine at day 5 after birth induced cortical damage and white matter damage, which was reduced in a dose-dependent manner by the AMPA receptor antagonists [3].
(S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.