[Leu8,D-Trp22,Tyr25] Somatostatin-28 is the analog of Somatostatin-28. Somatostatin-28 is a intestinal peptide containing somatostatin in its C-terminal portion[1][2].
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist[1]. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively[2]. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice[3].
2-Amino-N-phenylpropanamide (Compound 5b) hydrochloride is a Tocainid (HY-B1798) analog. Tocainid is an antiarrythmic agent[1].
QX-222 chloride, a trimethyl analogue of Lignocaine (HY-B0185), is a potent Na+ channel blocker[1][2][3].
Mu-6S-Palm-β-Glc is a fluorogenic substrate for palmitoyl-protein thioesterase (PPT). Mu-6S-Palm-β-Glc can be used for the research of neuronal ceroid lipofuscin disease in infants[1][2].
Fluphenazine dihydrochloride is a phenothiazine-class D1DR and D2DR inhibitor; used to deliver Fluphenazine to biological systems in studies probing the effects and metabolic fates of this commonly used dopamine antagonist.
Astressin is a potent corticotropin releasing factor (CRF) antagonist.
Deltorphin 2 is a selective peptide agonit for the δ opioid receptor.
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis [1][2].
Vocacapsaicin (CA-008) hydrochloride, a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride can provide meaningful and long-lasting pain relief[1].
Romifidine hydrochloride is an α2 adrenergic receptor agonist. Romifidine hydrochloride shows sedation effects in vivo[1][2].
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].
Lutein is a carotenoid with reported anti-inflammatory properties. A large body of evidence shows that lutein has several beneficial effects, especially on eye health[1].
D-threo-PPMP is a potent inhibitor of glucosylceramide (GlcCer) synthase. D-threo-PPMP can block karyokinesis and reduce cyst production[1][2].
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1[1].
Dehydrocrenatidine, a β-carboline alkaloid that can be isolated from Picrasma quassioides. Dehydrocrenatidine induces cell Apoptosis by activates ERK and JNK. Dehydrocrenatidine inhibits invasion and migration of cancer cells, it also suppresses neuronal excitability to exert analgesic effects[1][2].
(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].
Valrocemide (TV1901) is a promising antiepileptic drug candidate that shows a broad spectrum of anticonvulsant activity.
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.
N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). N-oleoyl-glutamine is a transient receptor potential (TRP) antagonist[1].
29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM[1].
Pamoic acid is a potent GPR35 agonist with an EC50 of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties[1][2].
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.
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.
UCSF648 (Compound 5A6-48) is a chemical probe for the 5-HT5A serotonin receptor. UCSF648 weakly activates ADRA2A and MTNR1A[1].
A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. IC50 value: 8 nMTarget: Nav1.8 sodium channelA 803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.