5-HT Receptor Agonist

D2R/D3R/5-HT1AR agonist 1 (compound 22b) is an orally active triple-target D2R/D3R/5-HT1AR agonist with EC₅₀ values of 1.29, 1.05 and 153.5 nM. D2R/D3R/5-HT1AR agonist 1 can improve the behavioral disorders induced by MPTP (HY-W114750) and exerts anti-depression effect. D2R/D3R/5-HT1AR agonist 1 can be used for the research of Parkinson's disease and depression.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC₅₀ = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC₅₀ = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.

4-Hydroxy MPT (4-OH-MPT), a serotonergic hallucinogen, is a 5-HT2A and 5-HT2B receptors agonist with EC₅₀ values of 3.82 nM and 3.4 nM, respectively.

PRX-03140 is a selective, blood-brain-barrier permeable 5-HT4 receptor agonist with a K_i value of 110 nM against rat brain 5-HT4 receptor. PRX-03140 can increase cortical ACh and histamine levels. PRX-03140 can be used in the research of Alzheimer's disease.

(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

Donitriptan hydrochloride (F-11356) is a potent, high efficacy agonist at 5-HT_1B/1D receptors with pK_is of 9.4 and 9.3, respectively.

2-(1-Piperazinyl)pyrimidine-d₈ is the deuterated-labeled 2-(1-Piperazinyl)pyrimidine (HY-W004464). 2-(1-Piperazinyl)pyrimidine is an orally effective α₂-adrenoceptor antagonist and 5-HT1A receptor agonist. 2-(1-Piperazinyl)pyrimidine is an in vivo metabolite related to buspirone. 2-(1-Piperazinyl)pyrimidine modulates excitatory synaptic transmission in the hippocampus and the release of monoamine transmitters such as norepinephrine and 5-HT by blocking α2-adrenoceptor and activating 5-HT1A Receptor. 2-(1-Piperazinyl)pyrimidine is used in research on psychiatric disorders such as anxiety and depression.

UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT_5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT_5AR.

Rizatriptan-d₆ (benzoate) is the deuterium labeled Rizatriptan benzoate. Rizatriptan benzoate is the agonist for 5-HT_1B and 5-HT_1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system^.

CGS 12066 (dimaleate) dimaleate is a selective 5-HT_1B receptor agonist with an IC₅₀ of 51 nM.

Rizatriptan (MK 462 free base) is an orally active 5-HT_1B/5-HT_1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache.

Sumatriptan hydrochloride (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research.

Org 12962 hydrochloride is a potent, selective and efficacious 5-HT_2C receptor agonist and exhibits pEC₅₀ values of 7.01, 6.38 and 6.28 for 5-HT_2C, 5-HT_2A and 5-HT_2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.

WAY 629 is a potent and selective 5-HT_2C agonist with EC₅₀s of 426, 260000 nM for 5-HT_2C and 5-HT_2A, respectively. WAY 629 decreases feeding behavior.

WAY 208466 is a selective 5-HT6 receptor agonist with an EC₅₀ of 7.3 nM. WAY-208466 increases GABA levels following both acute and chronic administration in the dorsolateral frontal cortex of rat models with stereotaxic surgery. WAY 208466 can be used for anxiety-related disorders like obsessive compulsive disorder (OCD) research.

ML 10302 hydrochloride is a potent and selective 5-HT₄ receptor agonist, with an EC₅₀ of 4 nM. ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT₃ receptor in binding assay.

Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.

1192U90 is an antipsychotic agent, dopamine D₂ receptor antagonist as well as serotonin 5-HT_1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system.

LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.

5-HT2A agonist 6 (compound 2-6) is a 5-HT2A agonist with an EC₅₀ of 1.7 nM. 5-HT2A agonist 6 is used in the study of stress-related disorders, namely depression, anxiety, and post-traumatic stress disorder.