Ziprasidone amino acid (Ziprasidone Impurity C) is an impurity of Ziprasidone. Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity [1].
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy[1][2].
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system[1].
Rapastinel Trifluoroacetate is an NMDA receptor modulator with glycine-site partial agonist properties and currently in a phase II clinical development program as an adjunctive therapy for major depressive disorder.
Bromopride is a dopamine antagonist with prokinetic properties， widely used as an antiemetic.
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research[2][3].
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors[1][2].
Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].
Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects.Target: Opioid ReceptorTrimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain [1]. The major product from drug metabolism of trimebutine in human beings is nor-trimebutine, which comes from removal of one of the methyl groups attached to nitrogen. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract [2, 3].
Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine) with efficacy similar to cocaine. Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis[1].
[Met5]-Enkephalin, amide is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
Milameline is a muscarinic receptor agonist that improves cognition.
Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space[1][2].
8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity[1][2].
(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity[1].
BChE-IN-6 (compound 12) is a potent BChE inhibitor, with a Ki of 0.182 μM. BChE-IN-6 shows chelating capacity on Zn2+. BChE-IN-6 can be used for Alzheimer’s disease (AD) research[1].
Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist[1].
Bromerguride (2-Bromolisuride) is an analogue of the ergot dopamine agonist Lisuride (HY-12713). Bromerguride exhibits central antidopaminergic properties[1].
Chloralose is widely used in neuroscience and veterinary medicine as an anesthetic and sedative.
Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively[1].
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors[1].
SA 47 is a selective and potent inhibitor of fatty acid amide hydrolase (FAAH) and carbamate[1].
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions[1].
Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
α-Conotoxin PeIA is an analgesic α-conotoxin.α-Conotoxin PeIA inhibits the α6β4, α9α10 and α3β2 nAChR.α-Conotoxin PeIA is also a potent inhibitor of N-type calcium channel via GABAB receptor activation[1][2][3].
Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. Target: SSRIsDesvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis [1]. Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with desvenlafaxine, which could impact the metabolism of drugs metabolized via this enzyme. Desvenlafaxine exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5% [2].
Alosetron Hcl is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: Target: 5-HT ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.