Serotonergics - Antagonists

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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.
C0832 Clozapine N-oxide 5-HT2 serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC.
C238 S(−)-Cyanopindolol hemifumarate salt solid, ≥98% (HPLC) 5-HT1A/1B serotonin receptor antagonist; β3-adrenoceptor antagonist.
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.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
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.
human ... HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
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.
human ... KCNH1(3756)
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.
G5918 GR 113808 ≥98% (HPLC), solid GR 113808 is a 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
rat ... Htr3a(79246), Htr4(25324)
G5793 GR 127935 hydrochloride hydrate >98% (HPLC), powder Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
human ... HTR1B(3351), HTR1D(3352)
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.
L2411 LY-367,265 Antidepressant, inhibits the serotonin transporter; 5-HT2A serotonin receptor antagonist.
human ... HTR2A(3356)
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.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
rat ... Htr7(65032)
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.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR6(3362), HTR7(3363)
M137 Methysergide maleate salt solid Nonselective 5-HT1, 5-HT2, and 5-HT7 serotonin receptor antagonist; antimigraine.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
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.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152), HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
P0667 Parthenolide ≥98% (HPLC) Anti-inflammatory agent that inhibits NF-κB activation.
human ... ELA2(1991), IKBKG(8517), NFKB1(4790), NKAP(79576), NKRF(55922)
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.
R3030 Risperidone ≥98% (HPLC), powder Risperidone is an antipsychotic; serotonin-dopamine antagonist.
human ... DRD2(1813), HTR2A(3356), HTR2C(3358)
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.
human ... HTR2A(3356)
rat ... Adra1a(29412), Drd2(24318), Htr1a(24473), Htr2a(29595), Htr7(65032)
R140 Ro 04-6790 dihydrochloride solid Selective 5-HT6 serotonin receptor antagonist.
human ... HTR6(3362)
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.
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.
human ... HTR4(3360)
S0693 SB 204741 >98% (HPLC) 5-HT2B serotonin receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD5(1816), HTR1E(3354), HTR2A(3356), HTR2B(3357), HTR2C(3358)
rat ... Adra1a(29412), Gabra2(29706), Htr1a(24473), Htr2b(29581), Htr3a(79246)
S180 SB-206553 hydrochloride hydrate ≥98% (HPLC), solid Potent 5-HT2B/5-HT2C serotonin receptor antagonist.
human ... HTR2B(3357), HTR2C(3358)
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
S1194 SB-258585 dihydrochloride ≥98% (HPLC), powder 5-HT6 serotonin receptor antagonist.
S174 SDZ-205,557 hydrochloride solid Potent, selective 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
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.
human ... CHRNA3(1136), CHRNA4(1137), CHRNB2(1141), CHRNB4(1143), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
rat ... Chrna7(25302), Drd2(24318), Htr1a(24473), Htr3a(79246)
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.
human ... HTR1A(3350)
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.
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.