Catalog No.
Product Name
Application
Product Information
Product Citation
- Nebivolol hydrochloride is t a highly selective antagonist of the β1-adrenoceptor (Ki = 0.88 nM, β2-adrenoceptor Ki = 48 nM).
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
5-HT Receptors/D2 dopamine receptor antagonist
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. - Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer
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5-HT Receptors antagonist
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy. -
alpha-1 adrenergic agonist
Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride. -
Dopamine Receptor antagonist
Paliperidone(Invega) is an atypical antipsychotic.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI. -
Dopamine Receptor Agonist
Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS). -
5-HT2C receptor antagonist
Puerarin is one of several known isoflavones. Puerarin is a 5-HT2C receptor and benzodiazepine site antagonist. Puerarin is being investigated as a self-microemulsifying drug delivery system.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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MT1/MT2-Receptor Agonist
Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor. -
α2 adrenergic agonist
Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist. - Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism.
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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Adrenergic Receptor agonist
Salbutamol sulfate (Albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. -
α1-adrenoceptor antagonist
Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). -
Adrenergic Receptor agonist
Synephrine (Oxedrine) is an amine compound commonly used for weight loss. -
Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
- Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder.
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5-HT Receptor agonist
Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo. -
mast cell stabilizer
Nedocromil is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade. -
LTD4 receptor antagonist
Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist. -
ETA-receptor Antagonist
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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SMO Antagonist
LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein. -
neurokinin-1 receptor antagonist
Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist. -
Opioid Receptor agonist
ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM. -
Opioid Receptor antagonist
JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.- Lihao Gu, .et al. , Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. , Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). -
H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. -
Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
- Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
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AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
CaSR antagonist
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. -
5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
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5HT1A antagonist
WAY-100635 was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor.
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Opioid Receptors agonist
BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM). -
Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively.
