mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively[1].
Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is an impurity of Rivastigmine. Rivastigmine is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively[1][2].
Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM[1].
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research[1][2].
D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders[1].
Homatropine hydrochloride is an orally active anticholinergic agent that rapidly dilates pupils and has cycloplegic effects. Homatropine hydrochloride also has antitussive activity. Homatropine hydrochloride can be used in research on eye diseases and coughs[1].
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1)[1].
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels[1]. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy[2]. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied[4].
4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling[1].
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property[1][2].
E-3620 is a potent 5-HT3 receptor antagonist. E-3620 can be used for the research of dyskinesi and gastrointestinal motility[1][2].
MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent[1].
Lenperone hydrochloride (AHR 2277) is an antipsychotic compound and a dopamine antagonist. Lenperone hydrochloride reduces gastroesophageal sphincter pressure of healthy dogs. Lenperone hydrochloride can be used for neurological disease research[1][2].
A potent, subtype-selective α3β4 nAChR partial agonist with Ki of 0.62 nM; selectively activates receptors containing β4- but not β2-subunits, shows no efficacy at α4β2 receptors and only marginal efficacy at α4β4 receptors expressed in oocytes; enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment.
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors[1][2][3].
Sarcosine-d3 (N-Methylglycine-d3) is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
Rosmarinic acid racemate is the racemate of Rosmarinic acid. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.IC50 value: 0.82 nM/3.14 nM (5-HT1B/5-HT1D, Ki) [1]Target: 5-HT1B/5-HT1D in vitro: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) [1]. Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery [2].in vivo: Eletriptan (<1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (<300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater [3]. Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats [4].
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface[1].
3-AQC, a piperazinylquinoxaline derivative, is a potent and competitive 5-HT3 receptor antagonist[1].
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist.
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat[1].
Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder[1][2].
Naratriptan-d3 is the deuterium labeled Naratriptan[1]. Naratriptan is a selective 5-HT1 receptor subtype agonist[2].
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors[1].
DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14)[1].
UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4[1][2].
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention[1].
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].