Fenoldopam (SKF 82526) hydrochloride is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam hydrochloride shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis[1][2][3].
Chlorpromazine D6 hydrochloride is the deuterium labeled Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.
VU0467485 (VU-0467485, AZ13713945) is potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator with EC50 of 78.8 nM (hM4); possesses robust in vitro M4 PAM potency across species and in vivo efficacy in preclinical models of schizophrenia.
BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM)[1].
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDAR. TCN 201 antagonism is dependent on the GluN1-agonist concentration. TCN 201 allows pharmacological identification of native GluN2A-containing NMDAR populations[1].
VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).IC50 value: 477 ± 172 nM (EC50) [1]Target: M1in vitro: VU0357017 is a M1-selective agonists that appear to activate M1 through actions at an allosteric site. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. [1] VU0357017 is a potent and efficacious M1 agonist, selective versus M2 M5 family members and allosteric agonist. VU0357017 is a highly selective M1 agonist suggests that these compounds are unlikely to act at the highly conserved orthosteric site on M1 and are more likely to act as allosteric agonists. [2] VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 significantly enhances threshold Θ-burst LTP and VU0364572 induces LTD at the Schaffer collateral-CA1 synapse of rodent hippocampal slices. [3]in vivo: VU0357017 has robust efficacy in improving hippocampal-dependent learning in rats. VU0357017 enhances performance in Morris water maze and contextual fear conditioning in rats. [3]
Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit[1].
μ opioid receptor agonist 3 (compound 20) is a potent μ opioid receptor (µOR) agonist with an EC50 of 0.87 nM. μ opioid receptor agonist 3 has the potential for pain and neuropsychiatric indications research[1].
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
Phenglutarimid is an anticholinergic used as an antiparkinsonian agent.
CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.IC50 value:Target: AMPAR agonistin vitro: Treatments with the ampakine CX614 markedly and reversibly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal slices [1]. in contrast to cyclothiazide or IDRA 21, the Ampakine CX546 binds specifically to the agonist bound nondesensitized receptor, most likely acting by destabilizing the desensitized receptor conformation [2]. In binding tests, CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective [3]. in vivo: Intraperitoneal injections of CX546 increased hippocampal BDNF mRNA levels in aged rats and middle-aged mice [1]. Administration of the positive modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptors (AMPAR), CX546, during the conditioning phase only, improved the disrupted LI in mGluR5 knockout mice and facilitated LI in control C57BL/6J mice, given extended number of conditioning trails (four conditioning stimulus-unconditioned stimulus) [4].
9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 µM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo[1].
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats[1][2].
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders[1].
GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra[1][2].
Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively[1].
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1[1][2].
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction[1].
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM)[1][3]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM[2]. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta[4]. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation[5].
Trimethobenzamide (Ro 2-9578 free base) is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting[1].
ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM[1][2].
5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptors agonist[1][2][3].
BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM). BP 897 exhibits selective inhibition of cocaine-seeking behavior[1].
Schisantherin B is a natural product.
Vanoxerine (GBR12909) is a potent and selective DRI (Dopamine reuptake inhibitor).IC50 value:Target: Dopamine reuptake inhibitorAt a cellular level, vanoxerine acts to block cardiac ion channels. Vanoxerine is a multichannel blocker, acting on IKr (potassium), L-type calcium and sodium ion channels.[14] By blocking these specific channels, there is a prolongation of the action potential of the cell, preventing reactivation by a reentrant circuit. The block is strongly frequency dependant: as the pacing of the heart increases so does the frequency of ion channel blocking by vanoxerine. Vanoxerine is a potentially effective treatment for cardiac arrhythmias. A significant cause of cardiac arrhythmias is reentry, an electrophysiologic event in which the proliferating signal that refuses to terminate, and endures to reexcite the heart after the refractory period.
BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection[1].
5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].
Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug.Target: nAChRAdiphenine decreased the frequency of ACh-induced single-channel currents. adiphenine decreased cluster duration (36-fold at 100 micromolxL(-1)). adiphenine did not change amplitude but increased the decay rate (IC(50)= 15 micromolxL(-1)) [1]. Adiphenine was administered in3H-labelled form in doses of 15 u.mole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured [1]. The elimination of the3H -labelled compound from the plasma was monophasic with a half-life of 13 minutes. The unchanged drug was detectable in the plasma for 30 minutes after the injection. The time course of brain levels of unchanged drug paralleled that found in the plasma with a half-life of 9 to 12 minutes. In all experiments, brain and plasma levels of unchanged adiphenine correlate highly [2].
YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92±0.22 and 2.64±0.30 nM for Notch and APPL cleavage, respectively.