Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent 5-HT2C agonist and 5-HT2B antagonist with an EC50 of 32 μM and an IC50 of 27 μM for 5-HT2C and 5-HT2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression[1][2].
Urapidil-d4 is the deuterium labeled Urapidil[1]. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist[2].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex[1]. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects[2].
WAY-181187 (SAX-187) hydrochloride is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM[1]. WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2].
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect[1].
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. Methylergometrine can be used as oxytocin and has protective effect on postpartum hemorrhage[1][2][3].
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK 293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects[1][2].
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors[1][2].
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia[1][2][3].
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia[1][2].
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia[1].
Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used to treat for cognitive disorders associated with Alzheimer＇s disease[1][2][3].
Desmethyl cariprazine is an active metabolite of Cariprazine[1]. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM)[2].
Tropanserin is a serotoninergic active compound, as well as a 5HT3 receptor antagonist. Tropanserin modulates Cardio-respiratory reflex effects of an exogenous serotonin challenge[1].
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors[1].
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-hydroxytryptamine (5-HT)2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].
Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1]Target: 5-HT3 receptorin vitro: In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT [1].in vivo: Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion [2]. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation [3].Clinical trial: Effect of External Heat on a Transdermal Granisetron Patch in Pharmacokinetics (PK) of Healthy Subjects. Phase 1
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5±1.1 nM.
Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM[1]. Neuroprotective effects[2].
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties[1][2][3].
Alosetron D3 Hcl is deuterium labeled Alosetron, which is a serotonin 5HT3-receptor antagonist.
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.The reference for administration is 10 mg/kg.
Dimethothiazine (Dimetotiazine; Fonazine) is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine can be used to research hemicrania and spasticity[1][2][3].
Alosetron 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.
5-HT3 antagonist 2 is a 5-HT3 receptor antagonist.
FR260010 free base is a selective 5-HT2C receptor antagonist, with a Ki value of 1.1 nM[1].