Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate (MCI-9042) increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease[1].
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM[1][2][3].
Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α，5-HT1β and 5-HT2，respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].
Almotriptan is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan 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].
Cyclobenzaprine-d6 (hydrochloride) is deuterium labeled Cyclobenzaprine (hydrochloride).
(S)-Bexcaserin (compound 2) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases[1].
AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia[1][2][3].
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].
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.
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].
Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties[1].
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity[1][2]. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM)[2].
Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).IC50 Value:Target: 5-HT3 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.
NLX-204 (NLX204) is a potent, selective, ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pEC50 of 9.37; shows promising pharmacokinetic profile, also robustly stimulates ERK1/2 phosphorylation in rat cortex and showed highly potent (MED=0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.
Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].
Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. IC50 Value: 4.2 nM(Ki)Target: 5-HT ReceptorAripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
Mirtazapine D3 (Org3770 D3; 6-Azamianserin D3) is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].
Methylergometrine maleate (Methylergonovine maleate) is an ergot alkaloid and an active metabolite of Methysergide with vasoconstrictive and uterotonic activity. Methylergometrine maleate is a potent, selective and orally active 5-HT receptors antagonist with a pA2 value of 9.6. Methylergometrine maleate has antimigraine and dopaminergic activity. Methylergometrine maleate can used for the prevention and control of postpartum hemorrhage[1][2][3].
Metoclopramide-d3 is deuterium labeled Metoclopramide. Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis[1][2].
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].
Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity[1][2].
UCSF686 is a probe with which to study the function of the 5-HT5AR. UCSF686 loses affinity at 5-HT5AR (>10 000 nM) but not at 5-HT1AR, 5-HT2BR, and 5-HT7R. UCSF686 controls for off-target effects[1].
Nefazodone hydrochloride is an antidepressant drug.
Naratriptan D3 Hydrochloride is the deuterium labeled Naratriptan, which is a selective 5-HT1 receptor subtype agonist.
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats[1][2].
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
(Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.