SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
Dopamine serotonin antagonist-1 is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
Vilazodone (EMD 68843; SB 659746A) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.IC50 value:Target: SSRI; 5-HT1AVilazodone represents another option for the treatment of MDD. Vilazodone appears to have a favourable weight-gain profile based on short-term studies. Sexual side-effects were not consistently demonstrated when assessed using clinical rating scales but spontaneously reported AEs related to sexual functioning were observed. Additional controlled data regarding long-term efficacy and effectiveness will help characterise this new agent when used in maintenance treatment.
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
Clomipramine D3 hydrochloride is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant[1].
Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.Target: SSRIsFluvoxamine is effective in inhibiting 5-ht uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted [2]. Fluvoxamine was less potent at decreasing ethanol self-administration when food was available concurrently versus when ethanol was available in isolation [ED50: 4.0 (2.7-5.9) and 5.1 (4.3-6.0)]. Effects on food were similar under each condition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduled food reinforcement [3].Clinical indications: Depression; Obsessive compulsive disorder; Social phobia FDA Approved Date: December 5, 1994Toxicity: Anorexia, Constipation, Dry mouth, Headache, Nausea, Nervousness, Skin rash, Sleep problems, Somnolence, Liver toxicity, Mania, Increase urination, Seizures, Sweating increase, Tremors, or Tourette's syndrome.
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1[1].
Clovoxamine (DU23811) (Compound 35) has binding affinity for serotonin transporter (SERT) (Ki: 61 nM). Clovoxamine is a 5-HT and norepinephrine reuptake (NE) re-uptake inhibitor. Clovoxamine is an antidepressant[1][2][3].
Vortioxetine is a 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.
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
Clomipramine (Chlorimipramine) is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
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].
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.
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).
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].
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.
Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs[1].
Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities[1][2][3].
Dapoxetine-d6 is the deuterium labeled Dapoxetine[1]. Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE)[2].
Fluvoxamine maleate is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.Target: SSRIsFluvoxamine (maleate) is the maleate salt form of fluvoxamine, which is effective in inhibiting 5-HT uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted [2]. Fluvoxamine was less potent at decreasing ethanol self-administration when food was available concurrently versus when ethanol was available in isolation [ED50: 4.0 (2.7-5.9) and 5.1 (4.3-6.0)]. Effects on food were similar under each condition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduled food reinforcement [3].Clinical indications: Depression; Obsessive compulsive disorder; Social phobia " FDA Approved Date: December 5, 1994Toxicity: Anorexia, Constipation, Dry mouth, Headache, Nausea, Nervousness, Skin rash, Sleep problems, Somnolence, Liver toxicity, Mania, Increase urination, Seizures, Sweating increase, Tremors, or Tourette's syndrome.
Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant[1][2][3][4].
Milnacipran is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia.Target: SNRIMilnacipran (Ixel, Savella, Dalcipran, Toledomin) is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the USA, but it is in other countries.Milnacipran inhibits the reuptake of serotonin and norepinephrine in an approximately 1:3 ratio, respectively; in practical use this means a relatively balanced action upon bothneurotransmitters. Increasing both neurotransmitters concentration simultaneously works synergistically to treat both depression and fibromyalgia. Milnacipran exerts no significant actions onH1, α1, D1, D2, and mACh receptors, as well as on benzodiazepine and opioid binding sites. Milnacipran is well absorbed after oral dosing and has a bioavailability of 85%. Meals do not have an influence on the rapidity and extent of absorption. Peak plasma concentrations are reached 2 hours after oral dosing. The elimination half-life of 8 hours is not increased by liver impairment and old age, but by significant renal disease. Milnacipran is conjugated to the inactive glucuronide and excreted in the urine as unchanged drug and conjugate. Only traces of active metabolites are found.
Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K+ channel (KV)4.3 is 17.3 μM.
Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor(SSRI).Target: SSRIDapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Premature ejaculation (PE) is the most common male sexual disorder, estimated to affect up to 30% of men. Dapoxetine is the only drug with regulatory approval for such an indication. The treatment of PE consists of primarily off-label use of oral selective serotonin reuptake inhibitors (SSRIs) via either on-demand or daily delivery.
Clomipramine D3 is the deuterium labeled Clomipramine, which is a highly selective inhibitor of serotonin reuptake.
Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD)[1].
DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.