Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
Glycyl-L-glutamic acid is a neurotrophic factor (NF) in vivo, and exerts function of maintenance of AChE content and activity. Glycyl-L-glutamic acid doesn’t act directly on AChE synthesis, and may prevent preganglionic neuronal degeneration[1][2].
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research[1].
Palonosetron Hcl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).IC50 Value:Target: 5-HT ReceptorPalonosetron is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy.
(R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.
Adoprazine, a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.IC50 Value: N/ATarget: Dopamine Receptor; 5-HT ReceptorAdoprazine is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia.
Indalpine (LM 5008) is a potent and selective 5-HT uptake blocker. Indalpine is potent in displacing 3H-5-HT bound to brain membranes with the IC50 of 36 μM[1]. Indalpine, two antidepressant agent[2].
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases[1][4].
Propionylpromazine is a dopamine receptor DRD2 antagonist. Propionylpromazine also is an effective tranquillizer. Propionylpromazine can be used in veterinary studies[1][2].
Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms[1][2][3].
4,4-Diphenylbutylamine shows affinity for the 5-HT2A and H1 receptors with Kis of 2589 and 1670 nM, respectively[1].
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent[1].
FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM.
Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].
Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE, respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50 Aβ=3.09 μM), tau aggregation (55% at 10 μM). Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s[1].
AM6701 is a potent FAAH/MAGL inhibitor (equipotent inhibitory IC50: 1.2 nM) with neuroprotective effects[1].
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.
2,6-Dimethyl-L-tyrosine (Dmt) is a tyrosine derivative that enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides[1].
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation[1].
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment[1][2].
PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities[1][2][3].
Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist[1][2].
Peptide E is a potent kappa opiate receptor agonist. Peptide E has opiate receptor binding activity with IC50 value of 0.39 μM. Peptide E can be used for the research of central nervous system[1][2].
Xanthohumol I, a chalkone, is a derivative of Xanthohumol (HY-N1067). Xanthohumol is a Cholinesterase (ChE) inhibitor, which inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) wih IC50s of 71.34 μM and 32.67 μM, respectively. The hydroxy compound of Xanthohumol (3-hydroxy-xanthohumol), also shoes inhibitory effect on AChE and BChE with IC50s of 51.25 μM and 63.07 μM[1].
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain[1].
SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes[1][2][3][4].
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer[1][2].
Verubecestat (MK-8931) is a beta-secretase 1 (BACE1) inhibitor under investigation for the treatment of Alzheimer's Disease.