human serotonin

Oleoyl Serotonin is an antagonist of hTRPV1 with an IC50 of 2.57 μM.

Ampreloxetine hydrochloride (TD-9855 HCl) has anti-inflammatory activity and is a potential compound for the treatment of depression and Alzheimer's disease.

DL-Tryptophan ((±)-Tryptophan) containing dipeptides are interesting ingredients for functional foods as a natural prevention for hypertension with reduced side effects due to its selective inhibition of the C-domain. Low thalamic Tryptophan uptake appears to be a strong, independent predictor of long survival in patients with previous glioma treatment.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki values of 0.55 μM in rabbit platelet membranes and 0.1 μM in guinea pig cerebellum membranes.

Imipramine (Dimipressin) is an orally active Fascin1 inhibitor with antidepressant and antitumor activity.Imipramine inhibits the 5-hydroxytryptamine transporter (IC50: 32 nM), induces apoptosis, and induces autophagy in U-87MG glioma cells.Imipramine has neuroprotective and immunomodulatory activities, inhibits TNT, and is used to label brain blood vessels.Imipramine is a neuroprotective and immunomodulatory compound. Imipramine has neuroprotective and immunomodulatory activities, inhibits invasion and migration of TNBC cells, and can be used to study breast cancer and epilepsy.

SB399885 (SB 399885) is an effective, brain penetrant, and orally active antagonist of SR-6. It shows 200-fold selectivity for SR-6 over other serotonin receptors (pKi: 9.11, 8.81, and 9.02 for human recombinant, native rat, and native human SR-6 receptors, respectively).

PF-05212377 (SAM-760) is an inhibitor of the serotonin receptor 5-HT6. It acts as a substrate for the human transport proteins P-gp non-BCRP. The compound has demonstrated blood-brain barrier permeability in non-human primates. PF-05212377 is utilized in research related to Alzheimers disease.

Trimipramine N-oxide, an active metabolite of the tricyclic antidepressant trimipramine, effectively inhibits human monoamine transporters for noradrenaline (hNAT), serotonin (hSERT), dopamine (hDAT), and the human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. It is utilized in the research of depression and anxiety [1].

(R)-Duloxetine Hydrochloride is a napthalenyloxy-substituted amine used in binding studies of human serum albumin along with (S)-Duloxetine. Unlike its enantiomer, it is not a very effective dual serotonin and norepinephrine reuptake inhibitor (SNRI).

Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of tylogenin was significantly greater than that of its parent glycosides, tylophoroside and acetyltylophoroside, and that of dexamethasone. The activity of tylogenin was found to increase with the incubation time. In the human leukocyte-dependent histamine release test model, the glycosides had only a minimal activity. In contrast, tylogenin, with a geom mean IC50 = 49 microM, exerted a significantly greater potency than dexamethasone. These results suggest that tylogenin could represent a new class of antiallergic agents.

6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism.

Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for hu

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.

(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6 via a 5- or 6-hydroxy duloxetine intermediate, followed by a catechol duloxetine intermediate. This compound effectively inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) across lipid membranes, with inhibition constants (Kis) of 266, 920, and 2,814 nM, respectively, for human transporters.

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

SCH 38519 is an isochromanequinone fungal metabolite originally isolated from Thermomonospora. It inhibits aggregation induced by thrombin , as well as inhibits serotonin secretion in human platelets (IC50s = 68 and 61 μg/ml, respectively). It inhibits the growth of various Gram-negative and Gram-positive bacteria (mean MICs = 122.1 and 0.92 μg/ml, respectively).

Izuforant (JW1601) (Compound 24) exhibits potent anti-inflammatory and anti-pruritic activities, with a binding affinity for human serotonin 3 receptor (h5-HT3R) and an IC50 value of 9.1 μM. It is also an orally active antagonist of histamine H4 receptor (H4R), showing an IC50 value of 36 nM against human H4R [1] [2].

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist with pKis of 8.19 and 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.

8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that enhances the spontaneous release of histamine by promoting the degranulation of mast cells in guinea pig and human intestinal preparations. By activating the serotonin signaling pathway, this compound demonstrates potential in regulating gastrointestinal functions and offers insight into the management and suppression of functional gastrointestinal disorders such as irritable bowel syndrome. Its effects in increasing histamine release could play a crucial role in gastrointestinal regulation.

Centanafadine hydrochloride (EB-1020 hydrochloride) is a dual inhibitor of norepinephrine (NE) dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been found in patients with schizophrenia, depression, and epilepsy.