Antagonists

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SML0346 Alosetron hydrochloride ≥98% (HPLC) Alosetron is a potent and highly selective antagonist of serotonin 5-HT3 receptors, nonselective cation channels found predominantly in the enteric nervous system of the gastrointestinal tract. These receptors are involved in the regulation of visceral pain, colonic transit and GI secretions that can contribute to the pathophysiology of irritable bowel syndrome (IBS). Alosetron is used clinically for treatment of women with severe diarrhea-predominant IBS.
    • A8106 Altanserin hydrochloride hydrate ≥98% (HPLC), solid Altanserin hydrochloride hydrate is a specific 5-HT2/serotonergic antagonist.
    • A7861 Asenapine maleate ≥98% (HPLC) Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.
    • B7188 Blonanserin ≥98% (HPLC) Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
    • C0832 Clozapine N-oxide 5-HT2 serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC.
    • SML0321 Cyamemazine ≥98% (HPLC) Cyamemazine belongs to the class of phenothiazine drugs. It is known to treat severe depression, schizophrenia and bipolar disorder.
    Cyamemazine is a potent antagonist of 5-HT2C and 5-HT3 receptors with antipsychotic and anxiolytic properties.
    • C4542 Cyclobenzaprine hydrochloride Cyclobenzaprine hydrochloride is a type of tricyclic skeletal drug, which is commonly used as a muscle relaxant. It is very effective in treating intractable pain of cervical and lumbar origin caused by skeletal muscle spasm. cyclobenzaprine hydrochloride inhibit tonic α-mononeuronal excitation mediated by descending serotonergic systems by interacting with serotonin receptors at the spinal cord level.
    Skeletal muscle relaxant; reduces muscle spasm by depression of brainstem neurons; 5-HT2 serotonin receptor antagonist.
    • C6022 Cyproheptadine hydrochloride sesquihydrate ≥98% (TLC), solid Cyproheptadine hydrochloride sesquihydrate is a serotonin receptor (5-HT2/5-HT1C) antagonist, H1 histamine receptor antagonist and an antipruritic. The inhibition of 5-HT by cyproheptadine improves cognitive function in schizophrenia disorder. Cyproheptadine is effective for treating functional gastrointestinal disorders (FGIDs). Food and Drug Administration (FDA) approved cyproheptadine, has antidepressant and antiplatelet functionality. It may be effective in treating thromboembolic disorders. Cyproheptadine inhibits lysine methyltransferase 7/9 (Set7/9) leading to a decrease in estrogen receptor (ERα) expression and growth arrest in breast cancer cells.
    • D9571 Dolasetron mesylate hydrate ≥98% (HPLC), powder Dolasetron mesylate hydrate is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.
    • SML0797   Flibanserin ≥98% (HPLC) Flibanserin is a 5-HT1A receptor agonist and 5-HT2A receptor antagonist. Flibanserin has high affinity for human 5-HT1A receptors (Ki = 1 nm) and lower affinity for 5-HT2A (Ki = 49 nm) and D4 (Ki = 4–24 nm) receptors, and negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin was investigated as a novel, non-hormonal treatment for pre-menopausal women with Hypoactive Sexual Desire Disorder (HSDD). Flibanserin. Recently, Flibanserin was found to reduce L-DOPA-induced dyskinesia in a model of Parkinson′s Disease.
    • G5918 GR 113808 ≥98% (HPLC), solid GR 113808 is a 5-HT4 serotonin receptor antagonist.
    • G5793 GR 127935 hydrochloride hydrate >98% (HPLC), powder Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
    • G3796 Granisetron hydrochloride ≥98% (HPLC), solid Granisetron hydrochloride helps to block nausea/emesis and abdominal pain in irritable bowel syndrome, that is stimulated by chemotherapy.
    Granisetron hydrochloride is a serotonin 5-HT3 receptor antagonist and antiemetic.
    • SML1528 Iloperidone ≥98% (HPLC) Iloperidone is an atypical antipsychotic, a combined dopamine (D2) and serotonin (5HT2) receptor antagonist. Iloperidone targets a selective set of dopamine, serotonin and also norepinephrine receptor subtypes. Like similar atypical antipsychotics, Iloperidone has higher affinity for the 5-HT2A receptor (Ki < 10 nM) than for the D2 receptor (Ki = 10–100) nM). Iloperidone has high affinity for dopamine D3 (Ki < 10 nM) and lower affinity for other serotonin or dopamine subtypes. Unlike most atypical antipsychotics, Iloperidone also has high affinity for norepinephrine alpha1 receptors (Ki < 10 nM) which may contribute to the drug’s efficacy on mood and cognition.
    • S006 Ketanserin (+)-tartrate salt ≥97%, solid Ketanserin stimulates collagen synthesis and is involved in wound healing.
    Selective 5-HT2 serotonin receptor antagonist. Ketanserin significantly reduces nicotine self-administration in rats, supporting an unexpected involvement of serotonin in nicotine addiction.
    • L2411 LY-367,265 Antidepressant, inhibits the serotonin transporter; 5-HT2A serotonin receptor antagonist.
    • L6670 LY266097 ≥98% (HPLC), powder LY266097 is a selective 5HT-2B antagonist with a pKI of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity for 5-HT2B than the human 5-HT2C and 5-HT2A.
    • SML0115 MDL 11939 ≥98% (HPLC) MDL 11,939 is a potent, selective and orally active 5-HT2 receptor antagonist (ASTAR). Ki values values are in the low nanomolar range for 5-HT2A with over 100-fold selectivity over 5-HT2C receptors and low or no affinity for non-5-HT2 receptors or transporters.
    • M3668 Metergoline Antagonist at 5-HT1, 5-HT2, and 5-HT7 serotonin receptors; analgesic; antipyretic.
    • M149 Methiothepin mesylate salt ≥98% (HPLC), solid Methiothepin mesylate salt is a 5-HT1, 5-HT6, 5-HT7 serotonin receptor antagonist, which blocks serotonin autoreceptors.
    • M137 Methysergide maleate salt solid Nonselective 5-HT1, 5-HT2, and 5-HT7 serotonin receptor antagonist; antimigraine.
    • M2525 Mianserin hydrochloride Antidepressant; antagonist/inverse agonist at 5-HT2 serotonin receptors; also blocks the H1 histamine receptor and the α2 adrenoceptor.
    Mianserin is a tetracyclic compound with sedative property. It lacks anticholinergic activity and is not effective on serotoninergic mechanisms. Mianserin is eliminated post biotransformation as hydroxylation, N-oxidation and N-demethylation products.
    • M2946 Mosapride citrate salt dihydrate 5-HT4 receptor agonist and 5-HT3 receptor antagonist
    Mosapride is found effective against chronic gastritis, functional dyspepsia and gastro-oesophageal reflux disease. It is useful in treating many other symptoms associated with gastrointestinal disorders. Mosapride is known to improve digestive motility.
    • D5676 N-Desmethylclozapine Major metabolite of clozapine; potent 5-HT2 serotonin receptor antagonist and a ligand for the cloned 5-HT6 and 5-HT7 serotonin receptors. Also an allosteric potentiator of M1 muscarinic receptors.
    N-Desmethylclozapine serves as an agonist to muscarinic acetylcholine receptors, and is known to exert its antipsychotic action. It blocks synaptic transmission by antagonizing synaptic GABA (γ-aminobutyric acid) receptors.
    • O1141 Olanzapine ≥98% (HPLC) Olanzapine is a 5-HT2 serotonin and D1/D2 dopamine receptor antagonist.
    • O3639 Ondansetron hydrochloride dihydrate ≥98% (HPLC), powder 5-HT3 serotonin receptor antagonist
    Ondansetron, (3RS)-9-methyl-3-[(2-methyl-1H-imidazol-1-yl) methyl] 1,2,3,9-tetrahydro-4H-carbazol-4-one hydrochloride dehydrate acts as a selective 5-hydroxytryptamine type 3 (5-HT3) serotonin receptor antagonist. It is used as an antiemetic to control nausea and vomiting associated with chemotherapy and radiotherapy.
    • SML1195 Palonosetron hydrochloride ≥98% (HPLC) Palonosetron is a potent and selective 5-HT3 receptor antagonist (Aloxi) used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
    • P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
    Pipamperone, a butyrophenone derivative is a pharmacological chaperone and is a membrane-permeable dopamine receptor D4 (DRD4) antagonist. The affinity of pipamperone is higher for DRD4 and 5-hydroxytryptamine 2A receptor (5-HT2A) in comparison with DRD2. It may be useful therapeutic in treating behavioral disorders and psychomotor agitation symptoms.
    • B9688 Pizotifen ≥98% (HPLC) Pizotifen is a serotonin antagonist acting mainly at the 5-HT1, 5-HT2A and 5HT2C receptors with some antihistamine activity. It is used for the prevention of vascular headache including migraine and cluster headache.
    • Q3638 Quetiapine hemifumarate salt ≥98% (HPLC) Quetiapine hemifumarate is an atypical antipsychotic, a combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
    Quetiapine promotes oligodendrogenesis in vitro. It is used in treating depressive disorders.
    • SML1909   RS 23597-190 ≥98% (HPLC) RS 23597-190 is a high affinity 5-HT4-selective antagonist with in vitro and in vivo efficacy. RS 23597-190 is a 4-amino-5-chloro-2-methoxybenzoate that antagonizes 5-HT-mediated relaxation of carbachol-contracted rat oesphageal muscularis mucosae ex vivo (pA2 = 7.5) and prevents 5-HT-induced tachycardia (tachyarrhythmia) of anaesthetized micropigs in vivo (6 mg/kg RS 23597-190 and 3-10 &amp;mu;/kg 5-HT via i.v.) by targeting 5-HT4 with high affinity (pKB = 7.8) and selectivity, while exhibiting no efficacy against 5-methoxytryptamine-mediated 5-HT3 activation in guinea-pig ileum and displaying much reduced or little affinity toward 5-HT3 (pKi = 5.7/mouse NG108-15 cells and pKB &amp;lt;5/guinea-pig ileum), dopamine receptors (pKi &amp;lt;4/D1 &amp; &lt;3/D2), muscarinic receptors (pKi &lt;4.5 toward M1/2/3/4), 5-HT1A &amp; 5-HT2 (pKi <5.2).
    • R2533 RS-127445 hydrochloride ≥98% (HPLC), powder RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
    • SML0674   Ramosetron hydrochloride ≥98% (HPLC) Ramosetron hydrochloride is a potent serotonin 5-HT3 receptor antagonist with higher afinity for the 5-HT3 receptor than other currently available antagonists. Ramosetron is used clinically both as an antiemetic to treat nausea and vomiting following chemotherapy or after surgery, and in treatment of irritable bowel syndrome.
    Ramosetron is a tetra hydrobenzimidazole derivative, containing an indole ring. It inhibits colon contraction mediated by serotonin, competitively.
    • R3030 Risperidone ≥98% (HPLC), powder Risperidone is an antipsychotic; serotonin-dopamine antagonist.
    • R103 Ritanserin powder Potent 5-HT2A serotonin receptor antagonist/inverse agonist that crosses the blood-brain barrier.
    Ritanserin is a potent serotonin 2A receptor (5-HT2A) serotonin receptor antagonist/inverse agonist, which crosses the blood-brain barrier. It modulates 5-HT2A receptors and has been suggested to have antiparkinsonian effect. Ritanserin also impacts schizophrenia by modulating mood, cognition and negative symptoms.
    • R140 Ro 04-6790 dihydrochloride solid Selective 5-HT6 serotonin receptor antagonist.
    • R8782 Ro4368554 ≥98% (HPLC) Ro4368554 is a 5-HT6 receptor antagonist. RO4368554 acts selectively at 5-HT6 receptors where it binds with a greater than 100-fold selectivity over other monoamine receptor subtypes (-log M pKi = 9.4 at 5-HT6 and 7.1 at 5-HT2A).
    • C238 S(−)-Cyanopindolol hemifumarate salt solid, ≥98% (HPLC) 5-HT1A/1B serotonin receptor antagonist; β3-adrenoceptor antagonist.
    • S0693 SB 204741 >98% (HPLC) 5-HT2B serotonin receptor antagonist.
    • S8061 SB 242084 dihydrochloride hydrate ≥98% (HPLC), powder SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5
    • SML0853   SB 699551 dihydrochloride ≥98% (HPLC) SB 699551 dihydrochloride is also known as (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4′-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride). It is considered as a useful tool to explain the physiological roles of the 5-ht5A receptor.
    SB-699551 is a 5-HT5A receptor antagonist, (pKi = 8.3) with 100-fold selectivity over other 5-HT receptor populations. SB-699551 completely blocks 5-HT-induced [35S]GTPγS membrane binding in cells expressing recombinant guinea pig 5-HT-5A.
    • S3313 SB-204070 hydrochloride solid, ≥97% (HPLC) SB-204070 is a highly potent and specific antagonist of 4-HT4 receptor. It inhibits cholinergic and noncholinergic transmission and blocks the contractions of proximal colon in guinea pigs and relaxation of human colon circular smooth muscle.
    Selective 5-HT4 serotonin receptor antagonist.
    • S180 SB-206553 hydrochloride hydrate ≥98% (HPLC), solid Potent 5-HT2B/5-HT2C serotonin receptor antagonist.
    • SML1349 SB-207266 ≥98% (HPLC) SB-207266 is a potent, selective, orally active and long-acting 5-HT4 antagonist in vivo.
    • S1194 SB-258585 dihydrochloride ≥98% (HPLC), powder 5-HT6 serotonin receptor antagonist.
    • SML1807 SB-258719 ≥98% (HPLC) SB-258719 is a selective and potent 5-HT7 antagonist. SB-258719 reverses the hypothermic effect of 5-CT in mice.
    • S7389 SB-269970 hydrochloride powder, ≥98% (HPLC) SB-269970 is an anti-psychotic agent that shows high affinity for 5-HT7 receptors. It may be effective in treating cognitive disabilities and schizophrenia-like deficits.4 SB-269970 desensitizes and decreases the excitatory effects of 5-HT7 receptors in rat hippocampus.5
    Selective 5-HT7 serotonin receptor antagonist.
    • S5326 SB-271046A ≥98% (HPLC) The first potent and selective 5-HT6 antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated.
    • SML0604   SB-399885 hydrochloride ≥98% (HPLC) SB-399885 is a potent, selective, and orally active 5-HT6 receptor antagonist with greater than 200 fold selectivity over other 5-HT receptors. SB-399885 is brain penetrant and displays antidepressant and anxiolytic activity in rodent models.
    • S174 SDZ-205,557 hydrochloride solid Potent, selective 5-HT4 serotonin receptor antagonist.
    • S5451 Sarpogrelate hydrochloride ≥98% (HPLC) Sarapogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist. It exhibits analgesic effects in numerous animal studies.
    • T104 Tropisetron monohydrochloride solid, ≥98% (HPLC) 3-Tropanylindole-3-carboxylate hydrochloride is a selective 5-HT3 serotonin receptor antagonist.
    Tropisetron a selective serotonin 5-HT3 receptor antagonist is used mainly as an antiemetic to treat nausea and vomiting following chemotherapy . In the treatment of fibromyalgia syndrome (FMS) tropisetron reduced not only pain perception but also had a favourable effect on cardiac dysfunction during treatment.
    • W0270 WAY 161503 hydrochloride ≥98% (HPLC) The 5-HT2C receptors have been implicated in conditions including obesity, anxiety, depression, OCD, schizophrenia, migraine, nociception and erectile dysfunction.
    • W108 WAY-100635 maleate salt powder WAY-100635 maleate salt is a highly selective 5-HT1A serotonin receptor antagonist. It has an ability to inhibit brexpiprazole, an antipsychotic drug that regulates serotonin-dopamine activity.
    • SML0081 Zacopride hydrochloride hydrate ≥98% (HPLC) Zacopride is a sub-nanomolar antagonist of the serotonin 5-HT3 receptor that also displays agonist-like activity against 5-HT4 receptors. It is a potent anxiolytic in animal models, and also has strong antiemetic effects, and also increases aldosterone levels via activation of 5-HT4 receptor in the adrenal glands.