5-HT Receptor Ligand

GR119566X is a 5-HT₃ receptor ligand with a pK_i value of 8.80 against prufied 5-HT₃ receptor. GR119566X can be used for 5-HT₃ receptor purification.

Iloperidone carboxylic acid (P95-12113) is the metabolite of Iloperidone (HY-17410). Iloperidone carboxylic acid exhibits good affinity for 5-HT2A receptor with pK_i of 8.15, and moderate affinity for adrenergic receptor α1/α2B/α2C.

GR119566X dihydrochloride is a 5-HT₃ receptor ligand with a pK_i value of 8.80 against prufied 5-HT₃ receptor. GR119566X dihydrochloride can be used for 5-HT₃ receptor purification.

NBUMP is a 5-HT₁A receptor ligand with a 5-HT₁A receptor K_i of 0.1 nM, α₁-adrenergic receptor K_i of 46 nM, and a 5-HT₁A receptor-to-α₁-adrenergic receptor selectivity ratio of 460.NBUMP binds to the 5-HT₁A receptor with high affinity.NBUMP binds to the α₁-adrenergic receptor with lower affinity.

Altanserin is a 5-hydroxytryptamine (5-HT_2A ) selective radioligand. Altanserin delivers human serotonin. Altanserin can be used to study the biochemical and cellular mechanisms of vulnerability to extracellular 5-HT increase .

5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (K_i of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC₅₀ of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC₅₀ for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with K_i of 1903 nM.

5-HT1A modulator 4 (Compound 1) is a ligand of 5-HT receptors. 5-HT1A modulator 4 has K_i values of 2.18 μM and 19.7 μM for 5-HT_1A and 5-HT_2A, respectively.

5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT_2AR ligand with nanomolar affinity for 5-HT_2AR (K_i: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.

5,7-Dihydroxytryptamine creatinine sulfate (5,7-DHT) is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine creatinine sulfate can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine creatinine sulfate can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons.

AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT_1ₐ and 5-HT₁ᵦ receptors, with nanomolar binding affinity. AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease.

R 116712 is a highly selective and affinity 5-HT4 receptor ligand. R 116712 can prepare isotopic markers.

Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (K_i=198 nM), α2A adrenergic receptor (K_i=180 nM; EC₅₀=440 nM) and 5-HT_2A receptor (EC₅₀=172 nM, E_max=76%). Z8779877149 inhibits 5-HT reuptake and activates G_i and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.

5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λ_ex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons.

5,7-Dihydroxytryptamine (5,7-DHT) hydrobromide is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine hydrobromide can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine hydrobromide can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons.

PZ-1129 is a selective 5-HT7 receptor ligand with a K_i of 7 nM. PZ-1129 shows K_i values of 159 and 24 nM for 5-HT1A receptor and D2 receptor. PZ-1129 can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC₅₀ = 13.7 nM). PZ-1129 can be used for the research of emotional disorders, such as depression and bipolar disorder.

5-HT5AR/5-HT6R ligand-1 (Compound PP10) is a ligand for serotonin receptors, showing high affinity for 5-HT_5A and 5-HT₆ receptors, with K_i values of 59 nM and 96 nM, respectively. 5-HT5AR/5-HT6R ligand-1 exhibits certain antiproliferative activity against tumor cells and can be used in the study of cancer.

E-6837 is a selective and orally active 5-HT₆ receptor ligand. E-6837 demonstrates partial agonism at a presumably silent rat 5-HT₆ receptor and full agonism at a constitutively active human 5-HT₆ receptor by monitoring the cAMP signaling pathway. E-6837 induces hypophagia, reduces fat mass and body weight, and improves glycemic control. E-6837 can be used for the research of obesity.

Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis.

BMS-181101 (hydrochloride) is an orally active antidepressant. BMS-181101 (hydrochloride) can interact with a variety of central presynaptic and postsynaptic 5-HT receptors. BMS-181101 (hydrochloride) can be used in the research of diseases such as depression.

2-Methyl-N,N-dimethyltryptamine (2,N,N-TMT, compound 15) has binding affinity for serotonin (5-HT) receptor, with the pA2 of 6.04. 2-Methyl-N,N-dimethyltryptamine plays an important role in neurological disease research.