(S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
MK-212 (CPP) is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 can stimulate phosphoinositide hydrolysis in cerebral cortex[1].
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion[1][2].
Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.IC50 Value: Target: H2 receptorin vitro:in vivo: In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses [1]. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p less than 0.001) [2].
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively[1][3].Org-12962 displays antiaversive effects in a rat model of panic-like anxiety[2].
ICI 89406 is a selective β1 adrenergic receptor antagonist amenable to labelling with positron emitters, for PET[1][2].
(β-Ala8)-Neurokinin A (4-10), a neuropeptide, is a potent and selective NK-2 tachykinin receptor (Neurokinin Receptor) agonist[1].
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site[1]. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test[2].
Triamcinolone Acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone. Target: Glucocorticoid ReceptorTriamcinolone acetonide is a synthetic corticosteroid used to treat various skin conditions, to relieve the discomfort of mouth sores, and in nasal spray form, to treat allergic rhinitis. It is a more potent derivative of triamcinolone, and is about 8 times as potent as prednisone [1].
Trimebutine 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].
Peptide YY (pig) is a 36 amino acid gastrointestinal peptide, can be isolated from porcine duodenum. Peptide YY (pig) decreases appetite and food-intake by activation of the Y2 receptor. Peptide YY (pig) is present mainly in pancreatic endocrine cells with effect on both intestinal motility and the cardiovascular system[1][2][3].
S1PR1 agonist 2 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 2 has the potential for the research of autoimmune diseases (extracted from patent WO2021175225A1, compound 1)[1].
SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].
(Leu31,Pro34)-Peptide YY (human) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM[1].
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2].
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
LY210073 is a Leukotriene B4 (LTB4) receptor antagonist with an IC50 of 6.2 nM.
Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM)[1]. Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively[2]. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis[3].
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model[2].
Ranitidine bismuth citrate is an orally active Histamine H2-receptor antagonist with an IC50 of 3.3 μM. Ranitidine bismuth citrate has high selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate is a commonly used agent anti-Helicobacter pylori infection with an MIC90 value of 16 ng/L[1][2][3].
Talibegron hydrochloride (ZD2079 hydrochloride) is a potent β3-adrenoceptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. Talibegron hydrochloride has potent vasorelaxant effect[1].
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.Target: 5- HT ReceptorIC50 Value: in vitro: 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) [1]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response [2].in vivo: Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating [3]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg [4]. ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection [5]. Toxicity: Ondansetron may be safe in lower doses used to prevent nausea and vomiting in radiation treatment or postoperatively. However, as there is a report that a lower dose of ondansetron prolonged the QT interval in healthy volunteers, this needs to be clarified by the FDA [6].
PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect[1].
AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation[1][2].
SKF 82958 hydrobromide is a D1/D5 receptor full agonist. IC50 value:Target: D1/D5 receptorin vitro: Neuropeptide and immediate early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and preprodynorphin (PPD) and substance P (SP) gene expression in medium spiny neurons in the dorsal, and especially, in the ventral striatum. in vivo:Quantitative in situ hybridization was used to examine the contribution of muscarinic receptors to the transynaptic regulation of striatal gene expression induced by D1receptor activation. The acute injection of the full D1 agonist, SKF-82958, would induce PPD, SP and PPE mRNA expression in the intact rat striatum.
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU[1][2].
Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS)[1].
TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models[1].
SOS1-IN-8 is a potent SOS1 inhibitor with IC50s of 11.6 and 40.7 nM for SOS1-G12D and SOS1-G12V, respectively (WO2022017339A1, compound 2)[1].