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 ǰȳ  Ű   Pharmacology

Serotonin Receptor Small Molecules

Serotonin Receptor ʿ Small Molecules Ұմϴ.

TOCRIS
ǰ ϱ
μϱ





Agonists
Cat. No. Product Name / Activity
5584 Aripiprazole
High affinity D2 and 5-HT1A partial agonist; also 5-HT2A antagonist
3346 ATC 0175 hydrochloride
5-HT1A partial agonist; also 5-HT2B antagonist and MCH1 antagonist
1006 BMY 7378 dihydrochloride
5-HT1A partial agonist
0556 BP 554 maleate
Selective 5-HT1A agonist
0962 Buspirone hydrochloride
5-HT1A partial agonist
1080 (R)-(+)-8-Hydroxy-DPAT hydrobromide
Selective 5-HT1A agonist; enantiomer of 8-Hydroxy-DPAT hydrobromide (Cat. No. 0529)
0529 8-Hydroxy-DPAT hydrobromide
Selective 5-HT1A agonist; also has moderate affinity for 5-HT7
0797 8-Hydroxy-PIPAT oxalate
High affinity 5-HT1A agonist
1869 Ipsapirone
Selective 5-HT1A agonist
0411 MDL 73005EF hydrochloride
Potent and selective 5-HT1A partial agonist
1746 Nemonapride
5-HT1A agonist; also highly potent D2-like dopamine antagonist
0912 RU 24969 hemisuccinate
5-HT1A and 5-HT1B agonist
1771 S 14506 hydrochloride
Highly potent 5-HT1A agonist; displays unique binding mechanism
2854 Tandospirone hydrochloride
Selective 5-HT1A partial agonist
1772 Urapidil hydrochloride
5-HT1A agonist; also α1-adrenoceptor antagonist
6202 Vilazodone hydrochloride
Potent 5-HT1A partial agonist and SSRI; antidepressant
2491 Xaliproden hydrochloride
High affinity 5-HT1A agonist; orally active
Antagonists
Cat. No. Product Name / Activity
2806 Alprenolol hydrochloride
5-HT1A antagonist; also β-adrenoceptor antagonist
0993 Cyanopindolol hemifumarate
5-HT1A and 5-HT1B antagonist; also β-adrenergic antagonist
0933 MM 77 dihydrochloride
5-HT1A (postsynaptic) antagonist
3282 NAD 299 hydrochloride
Selective, high affinity 5-HT1A antagonist
0553 NAN-190 hydrobromide
5-HT1A antagonist
1060 (S)-(-)-Pindolol
5-HT1A and 5-HT1B antagonist; also β-adrenergic antagonist; more active enantiomer of pindolol (Cat. No. 0994)
1516 SDZ 21009
5-HT1A and 5-HT1B antagonist; also β-adrenoceptor antagonist
0631 Spiroxatrine
5-HT1A antagonist
1253 (S)-WAY 100135 dihydrochloride
Potent and selective 5-HT1A antagonist
4380 WAY 100635 maleate
Potent 5-HT1A antagonist; also D4 agonist
Ligands
Cat. No. Product Name / Activity
0412 MDL 72832 hydrochloride
Potent 5-HT1A ligand



Agonists
Cat. No. Product Name / Activity
0703 Anpirtoline hydrochloride
Highly potent 5-HT1B agonist; also 5-HT3 antagonist
0638 CGS 12066B dimaleate
5-HT1B agonist
1032 CP 93129 dihydrochloride
5-HT1B agonist
1317 CP 94253 hydrochloride
Potent and selective 5-HT1B agonist
3862 Eletriptan hydrobromide
5-HT1B and 5-HT1D agonist; orally active
1860 Eltoprazine hydrochloride
5-HT1 and 5-HT2C partial agonist
5136 Rizatriptan benzoate
Potent 5-HT1B and 5-HT1D agonist
3586 Sumatriptan succinate
5-HT1A, 5-HT1B and 5-HT1D agonist
4657 Zolmitriptan
Potent 5-HT1B/1D/1F agonist
Antagonists
Cat. No. Product Name / Activity
0993 Cyanopindolol hemifumarate
5-HT1A and 5-HT1B antagonist; also β-adrenergic antagonist
1477 GR 127935 hydrochloride
Potent and selective 5-HT1B and 5-HT1D antagonist
1054 GR 55562 dihydrochloride
5-HT1B antagonist
0992 Isamoltane hemifumarate
5-HT1B antagonist
3350 LY 393558
Dual 5-HT1B and 5-HT1D antagonist; also 5-HT re-uptake inhibitor
1413 NAS-181
Selective r5-HT1B antagonist; active in vivo
1060 (S)-(-)-Pindolol
5-HT1A and 5-HT1B antagonist; also β-adrenergic antagonist; more active enantiomer of pindolol (Cat. No. 0994)
1242 SB 216641 hydrochloride
Selective h5-HT1B antagonist
1221 SB 224289 hydrochloride
Selective 5-HT1B antagonist
1516 SDZ 21009
5-HT1A and 5-HT1B antagonist; also β-adrenoceptor antagonist



Agonists
Cat. No. Product Name / Activity
3783 CP 135807
Selective 5-HT1D agonist
3862 Eletriptan hydrobromide
5-HT1B and 5-HT1D agonist; orally active
0864 GR 46611
5-HT1D agonist
0781 L-694,247
5-HT1D agonist
2640 L-703,664 succinate
Selective 5-HT1D agonist
1985 PNU 142633
Highly selective 5-HT1D agonist
5136 Rizatriptan benzoate
Potent 5-HT1B and 5-HT1D agonist
3586 Sumatriptan succinate
5-HT1A, 5-HT1B and 5-HT1D agonist
4657 Zolmitriptan
Potent 5-HT1B/1D/1F agonist
Antagonists
Cat. No. Product Name / Activity
1207 BRL 15572 hydrochloride
Selective h5-HT1D antagonist
1477 GR 127935 hydrochloride
Potent and selective 5-HT1B and 5-HT1D antagonist
3078 LY 310762 hydrochloride
Selective 5-HT1D antagonist
3350 LY 393558
Dual 5-HT1B and 5-HT1D antagonist; also 5-HT re-uptake inhibitor



Agonists
Cat. No. Product Name / Activity
1129 BRL 54443
Potent 5-ht1E and 5-HT1F agonist



Agonists
Cat. No. Product Name / Activity
1129 BRL 54443
Potent 5-ht1E and 5-HT1F agonist
3079 LY 334370 hydrochloride
Selective 5-HT1F agonist
2451 LY 344864 hydrochloride
Potent and selective 5-HT1F agonist
4657 Zolmitriptan
Potent 5-HT1B/1D/1F agonist


Agonists
Cat. No. Product Name / Activity
2643 DOI hydrochloride
5-HT2A and 5-HT2C agonist
5171 NBOH-2C-CN hydrochloride
High affinity and selective 5-HT2A agonist
2201 PNU 22394 hydrochloride
5-HT2C agonist and 5-HT2A/2B partial agonist
2592 TCB-2
High affinity and potent 5-HT2A agonist
Antagonists
Cat. No. Product Name / Activity
1809 Altanserin hydrochloride
5-HT2A receptor antagonist
5584 Aripiprazole
5-HT2A antagonist; also D2 and 5-HT1A receptor partial agonist
4468 AT 1015
Long-acting 5-HT2A antagonist
0444 Clozapine
5-HT2A and 5-HT2C antagonist; also dopamine antagonist
4480 DV 7028 hydrochloride
Selective 5-HT2A antagonist; antithrombotic
4470 EMD 281014 hydrochloride
Selective 5-HT2A antagonist
4958 Eplivanserin hemifumarate
Potent and selective 5-HT2A antagonist
0523 4F 4PP oxalate
Selective 5-HT2A antagonist
2645 Fananserin
5-HT2A antagonist; also D4 antagonist
0908 Ketanserin tartrate
Selective 5-HT2A antagonist. Also antagonist at 5-HT1D
4173 MDL 100907
Potent and selective 5-HT2A antagonist
0870 MDL 11,939
5-HT2A antagonist
2495 Melperone hydrochloride
5-HT2A antagonist; also D2 antagonist; neuroleptic
1644 Mesulergine hydrochloride
5-HT2A and 5-HT2C antagonist; also D2-like partial agonist
2777 Nefazodone hydrochloride
5-HT2A antagonist; also 5-HT uptake inhibitor; antidepressant
4349 Olanzapine
5-HT2A antagonist; also D2 antagonist; atypical antipsychotic
4493 Paliperidone
5-HT2A antagonist; also D2 antagonist; atypical antipsychotic
2735 PNU 96415E
5-HT2A and D4 antagonist; antipsychotic
1742 R-96544 hydrochloride
Potent, selective 5-HT2A antagonist
2865 Risperidone
5-HT2A antagonist; also D2 antagonist; atypical antipsychotic
3739 Sarpogrelate hydrochloride
Selective 5-HT2A antagonist
0995 Spiperone hydrochloride
5-HT2A antagonist; also D2-like antagonist
6336 Trazodone hydrochloride
5-HT2A and α1 adrenoceptor antagonist; also enhances neural differentiation; antidepressant and neuroprotectant
3085 Ziprasidone hydrochloride
5-HT2A antagonist; also D2 antagonist; atypical antipsychotic
3996 Zotepine
5-HT2A antagonist; also D2 and H1 antagonist; atypical antipsychotic



Agonists
Cat. No. Product Name / Activity
1059 BW 723C86 hydrochloride
5-HT2B agonist
0875 m-CPP hydrochloride
5-HT2B and 5-HT2C agonist
0557 α-Methyl-5-hydroxytryptamine maleate
5-HT2B agonist
Antagonists
Cat. No. Product Name / Activity
3346 ATC 0175 hydrochloride
5-HT2B antagonist; also 5-HT1A partial agonist and MCH1 antagonist
4081 LY 266097 hydrochloride
Selective 5-HT2B antagonist
3077 LY 272015 hydrochloride
High affinity 5-HT2B antagonist; orally active
2993 RS 127445 hydrochloride
High affinity and selective 5-HT2B antagonist
1371 SB 200646 hydrochloride
5-HT2C/2B antagonist
1372 SB 204741
Potent, selective 5-HT2B antagonist
1661 SB 206553 hydrochloride
Potent and selective 5-HT2B and 5-HT2C antagonist; orally active
1374 SB 215505
5-HT2B/2C antagonist
1379 SB 221284
Potent and selective 5-HT2B and 5-HT2C antagonist
1375 SB 228357
5-HT2C/2B antagonist/inverse agonist
1255 SDZ SER 082 fumarate
Selective 5-HT2B/2C antagonist



Agonists
Cat. No. Product Name / Activity
3041 CP 809101 hydrochloride
Potent and selective 5-HT2C agonist
0875 m-CPP hydrochloride
5-HT2B and 5-HT2C agonist
2643 DOI hydrochloride
5-HT2A and 5-HT2C agonist
1860 Eltoprazine hydrochloride
5-HT1 and 5-HT2C partial agonist
3017 1-Methylpsilocin
Potent and selective 5-HT2C agonist
0941 MK 212 hydrochloride
5-HT2C agonist
3585 Org 12962 hydrochloride
Selective 5-HT2C agonist
2201 PNU 22394 hydrochloride
5-HT2C agonist and 5-HT2A/2B partial agonist
1854 Ro 60-0175 fumarate
Potent, selective 5-HT2C agonist
0925 SCH 23390 hydrochloride
5-HT2C agonist; also potent dopamine D1-like antagonist and Kir3 channel blocker
1801 WAY 161503 hydrochloride
Potent and selective 5-HT2C agonist
2173 WAY 629 hydrochloride
Selective 5-HT2C agonist
Inverse Agonists
Cat. No. Product Name / Activity
4508 S 32212 hydrochloride
5-HT2C inverse agonist; α2-adrenoceptor antagonist
3527 SB 243213 dihydrochloride
Selective 5-HT2C inverse agonist
Antagonists
Cat. No. Product Name / Activity
0444 Clozapine
5-HT2A and 5-HT2C antagonist; also dopamine antagonist
1007 N-Desmethylclozapine
5-HT2C antagonist
1644 Mesulergine hydrochloride
5-HT2A and 5-HT2C antagonist; also D2-like partial agonist
1050 RS 102221 hydrochloride
Selective 5-HT2C antagonist
1371 SB 200646 hydrochloride
5-HT2C/2B antagonist
1661 SB 206553 hydrochloride
Potent and selective 5-HT2B and 5-HT2C antagonist; orally active
1374 SB 215505
5-HT2B/2C antagonist
1379 SB 221284
Potent and selective 5-HT2B and 5-HT2C antagonist
1375 SB 228357
5-HT2C/2B antagonist/inverse agonist
2901 SB 242084
Selective 5-HT2C antagonist; brain penetrant
1255 SDZ SER 082 fumarate
Selective 5-HT2B/2C antagonist



Agonists
Cat. No. Product Name / Activity
0440 m-Chlorophenylbiguanide hydrochloride
Potent and selective 5-HT3 agonist
0558 2-Methyl-5-hydroxytryptamine hydrochloride
5-HT3 agonist/potent 5-HT6 ligand
0566 N-Methylquipazine dimaleate
5-HT3 agonist
0969 1-Phenylbiguanide hydrochloride
5-HT3 agonist
6426 PSEM 89S
PSAML141F,Y115F-5-HT3 chimeric ion channel agonist
0629 Quipazine dimaleate
5-HT3 agonist
0988 RS 56812 hydrochloride
5-HT3 partial agonist
3547 Serotonin hydrochloride
Endogenous 5-HT receptor agonist
1205 SR 57227 hydrochloride
Potent and selective 5-HT3 agonist
6866 uPSEM 817 tartrate
Highly potent and selective PSAM4-5-HT3 and PSAM4-GlyR agonist
Antagonists
Cat. No. Product Name / Activity
0666 3-AQC
5-HT3 antagonist
2759 B-HT 920
5-HT3 antagonist; also α2-adrenoceptor and D2 agonist
5629 Dolasetron mesylate
Potent and selective 5-HT3 antagonist
2903 Granisetron hydrochloride
5-HT3 antagonist
0640 MDL 72222
5-HT3 antagonist
2018 Mirtazapine
Potent 5-HT3 antagonist; also 5-HT2, H1 and α2 antagonist; antidepressant
2844 Mosapride citrate
5-HT3 antagonist and 5-HT4 agonist
2891 Ondansetron hydrochloride
Selective 5-HT3 antagonist
7038 Palonosetron hydrochloride New
Highly potent and high affinity 5-HT3 antagonist
0736 2-[1-(4-Piperonyl)piperazinyl]benzothiazole
5-HT3 antagonist; also 5-HT4 agonist
3287 Prochlorperazine dimaleate
5-HT3 antagonist; also D2 and nAChR antagonist
2037 SDZ 205-557 hydrochloride
5-HT3 and 5-HT4 antagonist
0641 Tropanyl-3,5-dimethylbenzoate
5-HT3 antagonist
2459 Tropisetron hydrochloride
Potent 5-HT3 antagonist; also α7 nAChR partial agonist
4532 VUF 10166
High affinity 5-HT3 antagonist
0380 Y-25130 hydrochloride
Potent and selective 5-HT3 antagonist
1795 Zacopride hydrochloride
Highly potent 5-HT3 antagonist; also 5-HT4 agonist
Modulators
Cat. No. Product Name / Activity
4700 PU 02
Negative allosteric modulator of 5-HT3 receptors
Ligand
Cat. No. Product Name / Activity
1015 RS 16566 dihydrochloride
5-HT3 ligand; shows affinity for zacopride binding site
Others
Cat. No. Product Name / Activity
0357 N-Acetyltryptamine
Serotonin N-acetyltransferase substrate
2813 D-Amphetamine sulfate
Induces 5-HT, dopamine and noradrenalin release
0767 Bifemelane hydrochloride
MAO-A and MAO-B inhibitor
0938 p-Chlorophenylalanine
Tryptophan hydroxylase inhibitor
3306 8-(3-Chlorostyryl)caffeine
MAO-B inhibitor. Also A2A antagonist
1095 (R)-(-)-Deprenyl hydrochloride
MAO-B inhibitor
2695 Dexfenfluramine hydrochloride
5-HT re-uptake inhibitor. Also stimulates 5-HT release
0474 Dihydroergocristine mesylate
5-HT antagonist; also partial agonist at adrenergic and dopaminergic receptors
0475 Dihydroergotamine mesylate
5-HT antagonist; also partial agonist at adrenergic and D2-like receptors
1132 Harmane
MAO-A and MAO-B inhibitor
2460 Lazabemide hydrochloride
Selective MAO-B inhibitor
4395 Moclobemide
Reversible MAO-A inhibitor
0610 Parthenolide
5-HT release inhibitor
0724 Pirlindole mesylate
MAO-A inhibitor
6425 PSEM 308 hydrochloride
PSAML141F,Y115F-5-HT3 chimeric ion channel agonist
4308 Rasagiline mesylate
Selective, irreversible MAO-B inhibitor
0723 Tetrindole mesylate
MAO-A inhibitor



Agonists
Cat. No. Product Name / Activity
4374 BIMU 8
Potent 5-HT4 agonist
1695 Cisapride
5-HT4 agonist; stimulates intestinal ACh release
3089 CJ 033466
Selective 5-HT4 partial agonist
3499 ML 10302 hydrochloride
Potent and selective 5-HT4 partial agonist
2844 Mosapride citrate
5-HT4 agonist and 5-HT3 antagonist
0736 2-[1-(4-Piperonyl)piperazinyl]benzothiazole
5-HT4 agonist; also 5-HT3 antagonist
0989 RS 67333 hydrochloride
5-HT4 partial agonist
0990 RS 67506 hydrochloride
5-HT4 partial agonist
4613 Tegaserod maleate
5-HT4 partial agonist
1795 Zacopride hydrochloride
5-HT4 agonist; also highly potent 5-HT3 antagonist
Antagonists
Cat. No. Product Name / Activity
1322 GR 113808
Potent and selective 5-HT4 antagonist
1658 GR 125487 sulfamate
Potent and selective 5-HT4 antagonist; active in vivo
0728 RS 23597-190 hydrochloride
5-HT4 antagonist
0991 RS 39604 hydrochloride
5-HT4 antagonist
0785 SB 203186 hydrochloride
5-HT4 antagonist
1373 SB 204070
Potent and selective 5-HT4 antagonist
2037 SDZ 205-557 hydrochloride
5-HT3 and 5-HT4 antagonist



Antagonists
Cat. No. Product Name / Activity
3188 SB 699551
Selective 5-ht5a antagonist
Others
Cat. No. Product Name / Activity
0458 5-Carboxamidotryptamine maleate
Has high affinity for 5-ht5A and 5-HT7. Also 5-HT1 agonist



Agonists
Cat. No. Product Name / Activity
2382 EMD 386088 hydrochloride
Potent 5-HT6 agonist
4337 ST 1936 oxalate
Selective, high affinity 5-HT6 agonist
5589 WAY 181187 oxalate
High affinity and selective 5-HT6 agonist
3904 WAY 208466 dihydrochloride
Selective 5-HT6 agonist
Antagonists
Cat. No. Product Name / Activity
3326 BGC 20-761
High affinity 5-HT6 antagonist
4208 MS 245 oxalate
High affinity 5-HT6 antagonist
3285 NPS ALX Compound 4a dihydrochloride
Potent and selective 5-HT6 antagonist
6748 PRX 07034
Potent and selective 5-HT6 antagonist
4964 R 1485 dihydrochloride
Selective and high affinity 5-HT6 antagonist
2911 Ro 04-6790
Potent and selective 5-HT6 antagonist
1961 SB 258585 hydrochloride
Potent, selective 5-HT6 antagonist
3368 SB 271046 hydrochloride
Selective 5-HT6 antagonist; orally active
3189 SB 399885 hydrochloride
Potent and selective 5-HT6 antagonist
3688 SGS 518 oxalate
Selective 5-HT6 antagonist
Others
Cat. No. Product Name / Activity
0590 Metergoline
Has moderate affinity for 5-HT6 and high affinity for 5-HT7. Also 5-HT1/5-HT2 antagonist
0558 2-Methyl-5-hydroxytryptamine hydrochloride
5-HT3 agonist/potent 5-HT6 ligand
0997 Mianserin hydrochloride
Has moderate affinity for 5-HT6. Also 5-HT2 antagonist



Agonists
Cat. No. Product Name / Activity
1968 AS 19
Potent 5-HT7 agonist
Antagonists
Cat. No. Product Name / Activity
5005 DR 4485 hydrochloride
High affinity and selective 5-HT7 antagonist; orally bioavailable
1523 LY 215840
5-HT2/5-HT7 antagonist
0937 Pimozide
High affinity 5-HT7 antagonist; also D2 antagonist
2726 SB 258719 hydrochloride
Selective 5-HT7 antagonist
1612 SB 269970 hydrochloride
Potent and selective 5-HT7 antagonist; brain penetrant
Others
Cat. No. Product Name / Activity
0458 5-Carboxamidotryptamine maleate
Has high affinity for 5-ht5A and 5-HT7. Also 5-HT1 agonist
0529 8-Hydroxy-DPAT hydrobromide
Has moderate affinity for 5-HT7; also 5-HT1A agonist
0590 Metergoline
Has moderate affinity for 5-HT6 and high affinity for 5-HT7. Also 5-HT1/5-HT2 antagonist


Inhibitors
Cat. No. Product Name / Activity
2341 A 80426 mesylate
5-HT uptake inhibitor and α2 antagonist
4456 Amitriptyline hydrochloride
5-HT and NA reuptake inhibitor (SNRI); also TrkA/B agonist
4357 Bicifadine hydrochloride
Noradrenalin, 5-HT and dopamine re-uptake inhibitor
2322 BTS 54-505 hydrochloride
Potent 5-HT and NA reuptake inhibitor (SNRI); active metabolite of sibutramine (Cat. No. 2290)
1427 Citalopram hydrobromide
Highly potent and selective 5-HT uptake inhibitor
0457 Clomipramine hydrochloride
5-HT reuptake inhibitor
2833 Cocaine hydrochloride
Inhibitor of monoamine transporters
4358 Dapoxetine hydrochloride
Selective serotonin reuptake inhibitor (SSRI)
2695 Dexfenfluramine hydrochloride
5-HT reuptake inhibitor; also stimulates 5-HT release
4798 (S)-Duloxetine hydrochloride
Potent 5-HT and NA reuptake inhibitor (SNRI); also blocks dopamine reuptake
4796 Escitalopram oxalate
Selective serotonin reuptake inhibitor (SSRI)
0927 Fluoxetine hydrochloride
5-HT reuptake inhibitor
1033 Fluvoxamine maleate
5-HT reuptake inhibitor
1588 Indatraline hydrochloride
Potent 5-HT uptake inhibitor; also inhibits dopamine and noradrenalin uptake
2545 Lofepramine
5-HT and NA reuptake inhibitor (SNRI)
3350 LY 393558
5-HT reuptake inhibitor; also 5-HT1B and 5-HT1D antagonist
2148 (±)-McN 5652
Potent, orally active 5-HT uptake inhibitor; also inhibits noradrenalin and dopamine uptake in vitro
3027 (±)-MDMA hydrochloride
Inhibitor of 5-HT and dopamine uptake; hallucinogenic
3286 Milnacipran hydrochloride
5-HT and NA reuptake inhibitor (SNRI)
2777 Nefazodone hydrochloride
5-HT uptake inhibitor; also 5-HT2A antagonist; antidepressant
2141 Paroxetine maleate
Highly potent and selective 5-HT uptake inhibitor
2395 Sertraline hydrochloride
5-HT reuptake inhibitor
2290 Sibutramine hydrochloride
5-HT and NA reuptake inhibitor (SNRI)
2175 Tetrabenazine
Potent inhibitor of vesicular monoamine transport; depletes 5-HT stores
2917 Venlafaxine hydrochloride
5-HT and NA reuptake inhibitor (SNRI)
6202 Vilazodone hydrochloride
Potent SSRI and 5-HT1A partial agonist; antidepressant
4194 WY 45233 succinate
5-HT and NA reuptake inhibitor (SNRI)
1767 Zimelidine dihydrochloride
Selective 5-HT uptake inhibitor
Others
Cat. No. Product Name / Activity
5763 (R)-Citalopram oxalate
Enantiomer of escitalopram oxalate (Cat. No. 1427)
3547 Serotonin hydrochloride
Endogenous substrate
1972 Tianeptine sodium salt
Selective facilitator of 5-HT uptake; antidepressant