Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively[1][2][3][4][5].
Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent[1]. Tesofensine is a CNS acting anti-obesity agent[2].
Milnacipran (1S-cis) hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI), used in the clinical treatment of fibromyalgia.
Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier[1].
Ansofaxine is a serotonin-norepinephrine reuptake inhibitor (SNRI) used for the research of depression[1].
Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE)[1].
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively[1]. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats[2].
rel-Paroxetine hydrochloride is a isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIsPipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment ofdepression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.
Fluoxetine hydrochloride is an antidepressant and a selective serotonin reuptake inhibitor.
DOV-216,303 is an antidepressant compound. DOV-216,303 inhibits the reuptake of norepinephrine (NE), serotonin (5‐HT), and dopamine (DA), with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. DOV-216,303 increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats[1][2][3].
Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).Target: SNRIDuloxetine (sold under the brand names Cymbalta, Ariclaim, Xeristar, Yentreve, Duzela, Dulane) is a serotonin-norepinephrine reuptake inhibitor(SNRI) manufactured and marketed by Eli Lilly. It is prescribed for major depressive disorder and generalized anxiety disorder (GAD). Duloxetine also has approval for use in osteoarthiritis and musculoskeletal pain. Duloxetine failed the US approval for stress urinary incontinence amidst concerns over liver toxicity and suicidal events; however, it was approved for this indication in Europe, where it is recommended as an add-on medication in stress urinary incontinence instead of surgery. It can also relieve the symptoms of painful peripheral neuropathy, particularly diabetic neuropathy, and it is used to control the symptoms of fibromyalgia.The main uses of duloxetine are in major depressive disorder, general anxiety disorder, stress urinary incontinence, painful peripheral neuropathy,fibromyalgia, and chronic musculoskeletal pain associated with osteoarthritis and chronic lower back pain. It is being studied for various other indications.
Milnacipran-d5 (hydrochloride) is deuterium labeled Milnacipran (hydrochloride).
Pseudoisocyanine (iodide) is a pan inhibitor of monoamine transporters and organic cation transporters with antidepressant-like activity[1].
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities[1].
Duloxetine is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). Target: SNRIsDuloxetine inhibits the reuptake of serotonin and norepinephrine in the central nervous system. Duloxetine is also considered a less potent inhibitor of dopamine reuptake. However, duloxetine has no significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and GABA receptors and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NA transporters. Duloxetine undergoes extensive metabolism, but the major circulating metabolites do not contribute significantly to the pharmacologic activity. Major depressive disorder is believed to be due in part to an increase in pro-inflammatory cytokines within the central nervous system. Antidepressants including ones with a similar mechanism of action as duloxetine, i.e. serotonin metabolism inhibition, cause a decrease in proinflammatory cytokine activity and an increase in anti-inflammatory cytokines; this mechanism may apply to duloxetine in its effect on depression but research on cytokines specific to duloxetine therapy is lacking [1]. The analgesic properties of duloxetine in the treatment of diabetic neuropathy and central pain syndromes such as fibromyalgia are believed to be due to sodium ion channel blockade [2].
Paroxetine maleate is a potent and selective inhibitor of SSRI. Paroxetine maleate is used in generalized anxiety disorder, post traumatic stress disorder, premenstrual dysphoric disorder and chronic headache research[1].
Imipramine hydrochloride inhibits serotonin transporter with an IC50 value of 32 nM in vitro.
Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.Target: SSRIsEscitalopram, the S-enantiomer of citalopram, belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Escitalopram may be used to treat major depressive disorder (MDD) and generalized anxiety disorder (GAD). Escitalopram has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of escitalopram is found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Escitalopram does not inhibit monoamine oxidase.
Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3].
Nardosinonediol (Tetrahydronardosinon) is a serotonin transporter (SERT) inhibitor[1].
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research[1][2][3].
Venlafaxine hydrochloride is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.Target: SNRIVenlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder (MDD), as a treatment for generalized anxiety disorder, and comorbid indications in certain anxiety disorders with depression. In 2007, venlafaxine was the sixth most commonly prescribed antidepressant on the U.S. retail market, with 17.2 million prescriptions.Venlafaxine is a bicyclic antidepressant, and usually categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI), but it has been referred to as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It works by blocking the transporter "reuptake" proteins for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin and norepinephrine. Additionally, in high doses it weakly inhibits the reuptake of dopamine, with recent evidence showing that the norepinephrine transporter also transports some dopamine as well, since dopamine is inactivated by norepinephrine reuptake in the frontal cortex. The frontal cortex largely lacks dopamine transporters; therefore, venlafaxine can increase dopamine neurotransmission in this part of the brain. Venlafaxine interacts with opioid receptors (mu-, kappa1- kappa3- and delta-opioid receptor subtypes) as well as the alpha2-adrenergic receptor, and was shown to increase pain threshold in mice. When mice were tested with a hotplate analgesia meter (to measure pain), both venlafaxine and mirtazapine induced a dose-dependent, naloxone-reversible antinociceptive effect following intraperitoneal injection. These findings suggest venlafaxine's seemingly superior efficacy in severe depression as narcotics become increasingly used as a measure of last resort for refractory cases.
Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine) with efficacy similar to cocaine. Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis[1].
Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM.