5-HT Receptor Agonist

(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT_2B receptor agonist (K_i: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca²⁺. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease.

Befiradol (NLX-112) is a highly selective 5-HT₁A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol attenuates sedative agent-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of sedative agent-induced analgesia and sedation in adult rats. Befiradol can be used in studies related to opioid-induced respiratory depression.

AS19 is a potent, selective 5-HT₇ receptor agonist with an IC₅₀ value of 0.83 nM and a K_i of 0.6 nM. AS19 is selective for 5-HT₇ over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.

cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (K_d=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Phenylbiguanide is a 5-HT₃ receptor selective agonist with an EC₅₀ of 3.0±0.1 μM.

Gepirone is a selective 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research.

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.

LY334370 is a selective 5-HT_1F receptor agonist with a K_i of 1.6 nM.

Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

Naratriptan (GR-85548A) hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.

PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT₄R) agonist. PF-04995274 has an EC₅₀ range of 0.26-0.47 nM for human 5-HT_4A/4B/4D/4E (K_i range of 0.15-0.46 nM), and has an EC₅₀ range of 0.59-0.65 nM for rat 5-HT_4S/4L/4E (K_i of 0.30 nM for rat 5-HT_4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.

CP-809101 hydrochloride is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and 5HT_2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.

5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT₅ and 5-HT₇ receptors agonist.

Remlifanserin (ACP-204) is a highly selective 5-HT2A inverse agonist. Remlifanserin is applicable to research related to Alzheimer's disease psychosis.

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate hydrate 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 hydrate has the potential for migraine research.

CP 93129 dihydrochloride is a potent 5HT_1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.

Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively.

WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a K_i of 2.2 nM and an EC₅₀ of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.

PNU-142633 is a high affinity, selective and orally active 5-HT_1D receptor agonist with K_is of 6 nM and > 18 000 nM for human 5-HT_1D receptor and human 5-HT_1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC₅₀ value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.