human serotonin

Centanafadine 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).

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).

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.

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.

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).

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.

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.

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

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.

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.

STOCK3S-30866 is a selective allosteric inhibitor targeting the human serotonin transporter (hSERT).

AZD1134 is an orally active, brain-penetrant, and highly selective 5-HT1B receptor antagonist with IC50 values of 2.9 nM (human) and 0.108 nM (guinea pig). It elevates synaptic serotonin levels in guinea pigs and holds potential for research in mental disorders such as depression and anxiety.

Levomilnacipran (F2696; (1R,2S)-milnacipran) is the enantiomer of milnacipran and acts as a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. It also serves as a human α-adrenergic receptor antagonist with an IC50 of 3.4 μM, as detailed in patent WO2013014263A1.

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).

SB 204741 is a selective 5-HT2B antagonist with high affinity and pKi value of 7.1.

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

N-desmethyl Zolmitriptan (DZT) is an active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist zolmitriptan . DZT is an agonist of 5-HT1B receptors that induces contraction of isolated human cerebral arteries (EC50 = 100 nM).

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).

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg/kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.

Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .

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.

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].