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 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 5-HT2/5-HT1C serotonin receptor antagonist; H1 histamine receptor antagonist; antipruritic.
    		 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.
    		 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), solid Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
    		 human ... HTR1B(3351), HTR1D(3352)
    • G0419 GR 55562 dihydrobromide >97% (HPLC), powder 5-HT1B/5-HT1D serotonin receptor antagonist
    		  
    • G3796 Granisetron hydrochloride ≥98% (HPLC), solid Granisetron hydrochloride is a serotonin 5-HT3 receptor antagonist and antiemetic.
    		  
    • L2536 LY-310,762 hydrochloride white powder Potent, selective 5-HT1D serotonin receptor antagonist.
    		 human ... HTR1D(3352)
    • 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.
    		 human ... ADRA2A(150), ADRA2B(151), ADRA2C(152), HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
    • M226 p-MPPF dihydrochloride solid Selective 5-HT1A serotonin receptor antagonist. More potent than p-MPPI.
    		 human ... HTR1A(3350)
    • N3529 NAN-190 hydrobromide Potent 5-HT1A serotonin receptor antagonist active in the nM range.
    		 human ... HTR1A(3350)
    • P0667 Parthenolide ≥98% (HPLC) Anti-inflammatory agent that inhibits NF-κB activation.
    		 human ... ELA2(1991), IKBKG(8517), NFKB1(4790), NKAP(79576), NKRF(55922)
    • P126 Pirenperone >97%, solid 5-HT2 serotonin receptor antagonist.
    		 human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
    • 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.
    		  
    • R103 Ritanserin powder Potent 5-HT2A serotonin receptor antagonist/inverse agonist that crosses the blood-brain barrier.
    		 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) 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)
    • S1068 SB-215505 solid, >98% (HPLC) Selective 5-HT2B serotonin receptor antagonist; 100-fold higher affinity at 2B versus 2C.
    		 human ... HTR2B(3357)
    • S8061 SB 242084 dihydrochloride hydrate ≥98% (HPLC), powder Selective 5-HT2c serotonin receptor antagonist; crosses the blood-brain barrier.
    		  
    • 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)
    • S8072 Sertindole ≥97.5% (HPLC) Sertindole is a 5-HT2 serotonin and D2 dopamine receptor antagonist and antipsychotic.
    		  
    • 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)
    • U108 S(−)-UH-301 hydrochloride solid Potent, selective 5-HT1A serotonin receptor antagonist; D2/D3 dopamine receptor agonist.
    		 human ... HTR1A(3350)
    • W108 WAY-100635 maleate salt powder WAY-100635 maleate salt is a highly selective 5-HT1A serotonin receptor antagonist.
    		 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.
    		  
    • Z2777 Ziprasidone hydrochloride monohydrate ≥98% (HPLC), solid Ziprasidone is an atypical antipsychotic; FDA approved for the treatment of schizophrenia.