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D101 (±)-DOI hydrochloride ≥98% (HPLC), solid (±)-DOI hydrochloride is a potent and selective 5-HT2 serotonin receptor agonist that crosses the blood-brain barrier, increases dopamine turnover and the treatment with DOI counteracted the expression of the nicotine-induced locomotor and neurochemical sensitization, but had no effect on nicotine-induced behavioral disinhibition. The responses to DOI provide evidence that of these receptors are abundant in the cortex, and show relatively lower levels in hippocampus and cerebellum.
N3288 (+)-Norfenfluramine hydrochloride ≥98% (HPLC), powder (+)-Norfenfluramine is the major hepatic metabolite of (+)-fenfluramine and is primarily responsible for the anorexic effect, as well as side effects; (+)-norfenfluramine causes vasoconstriction and a blood pressure increase in rats with normal blood; acts primarily on the cytoplasmic pool of serotonin; more potent than fenfluramine at inducing dopamine release.
D153 (R)(−)-DOI hydrochloride ≥98% (HPLC), solid Potent and selective 5-HT2 serotonin receptor agonist that crosses the blood-brain barrier; more potent enantiomer of ±-DOI hydrochloride.
H140 (R)-(+)-8-Hydroxy-DPAT hydrobromide ≥98% (HPLC), solid (R)-(+)-8-Hydroxy-DPAT is a full 5-HT1A serotonin receptor agonist; active enantiomer of (±)-8-hydroxy-DPAT.
C144 1-(3-Chlorophenyl)biguanide hydrochloride solid Very potent 5-HT3 serotonin receptor agonist.
125180 1-(3-Chlorophenyl)piperazine hydrochloride 99% 1-(3-Chlorophenyl)piperazine induces hypophagia in food-deprived and freely feeding rats. CPP has affinity for 11 neurotransmitter receptor binding sites in human brain membranes.
5-HT2c serotonin receptor agonist; metabolite of trazodone.
164216 1-Phenylbiguanide 98%  
SML0640 2-Methylserotonin maleate ≥95% (HPLC) 2-Methylserotonin is a selective full agonist at the 5-HT3 receptor.
C117 5-Carboxamidotryptamine maleate salt powder, ≥98% (HPLC) Agonist at 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 serotonin receptors.
M3196 5-MEO-DIPT hydrochloride hydrate 5-MeO-DIPT is a tryptamine derivative. In animal behavioral studies, 5-MeO-DIPT has been shown to produce behavioral effects that are substantially similar to those of LSD, both schedule I hallucinogens.
SML1484 Allyphenyline oxalate ≥98% (HPLC) Allyphenyline is a potent α2C-adrenoceptor/serotonin 5-HT1A receptor agonist and α2A-adrenoceptor antagonist that exhibits anxiolytic effect and antidepressant activity. Allyphenyline attenuates opioid and alcohol withdrawal symptoms including hyperlocomotion and anxiety.
SML1210   Almotriptan malate ≥98% (HPLC) Almotriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Almotriptan has low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower. Affinity for 5-HT(7) and 5-HT(1A) receptors was approximately 40 and 60 times lower than that for 5-HT(1B/1D) receptors, respectively.
BM0009   Avitriptan fumarate ≥98% (HPLC) Avitriptan fumarate is a serotonin 5HT-1B/1D-receptor agonist with anti-migraine activity.
B4063 BIMU8 hydrate ≥98% (HPLC) BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist. Serotonin (5-HT) is a major neurotransmitter that acts through a family of GPCRs and one ion channel. 5-HT4 receptor is GPCR expressed in many tissues, including brain, and modulates dopamine secretion, learning, and memory. BIMU8 is a full agonist at 5-HT4, but it binds differently than the endogenous ligand, 5-HT, shown through site-directed mutagenesis studies. It depolarizes neurons and was used to localize 5-HT4 to somatic but not dendritic regions of CA1 pyramidal neurons.
B173 BRL 54443 maleate salt solid Potent 5-HT1E/1F serotonin receptor agonist.
B175 BW 723C86 ≥98% (HPLC) 5-HT2B serotonin receptor agonist.
SML1670 Bifeprunox mesylate ≥98% (HPLC) Bifeprunox (DU-127,090) is an atypical antipsychotic. Bifeprunox is a dopamine D2 receptor (D2R) partial agonist that exhibits 5-HT1A agonist properties.
B7148 Buspirone hydrochloride 5-HT1A serotonin receptor agonist; anxiolytic.
C106 CGS-12066 maleate salt solid 5-HT1B serotonin receptor agonist.
PZ0121 CP-135807 ≥98% (HPLC) CP-135807 is a selective 5-HT1D agonist.
PZ0102 CP-93129 dihydrochloride hydrate ≥98% (HPLC) CP-93129 is a potent and selective 5-HT1B agonist.
SML0588 CP-94,253 dihydrochloride ≥98% (HPLC) CP-94,253 is a potent and selective serotonin 5-HT1B receptor agonist with approximately 25x and 40x selectivity over the closely related 5-HT1D and 5-HT1A receptors. Ki values are 89, 2, 860, 49 and 1,600 nM for 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D and 5-HT2 receptors respectively. CP-94,253 was found to be anxiolytic in animal models; dose-dependently enhanced reinforcing effects of cocaine (self-administration);and reduced food intake.
SML0139 EMD386088 ≥98% (HPLC) EMD-386088 is a potent serotonin 5-HT6-specific agonist. The IC50 for competition of LSD from 5-HT6 expressed in HEK cells is 7.4 nM, and the EC50 for stimulating cAMP production is 1 nM. EMD-386088 is inactive against other HT receptors except 5-HT3 (IC50 = 34 nM).
EMD386088 effectively reverses cholinergic and glutataminergic-induced deficits in cognitive functions. It may be a therapeutic option in improving associated learning in Alzheimer′s disease and schizophrenia. EMD386088 also exhibits anti-depressant and anxiolytic effects in rats.
PZ0011 Eletriptan hydrobromide ≥98% (HPLC) Eletriptan hydrobromide is a serotonin 5-HT1B/1D receptor agonist; second generation anti-migraine drug.
SML1526 Eltoprazine hydrochloride ≥98% (HPLC) Eltoprazine hyrochloride is a serotonin 5-HT1A/1B receptor agonist that has been shown to reduce L-DOPA-induced dyskinesias in in experimental models of Parkinson′s Disease and in human patients. It has Ki values for 5-HT1A, 5-HT1B and 5-HT1C receptors of 40 nM and 52 nM, respectively.
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.
SML1291 Frovatriptan succinate monohydrate ≥97% (HPLC) Frovatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Frovatriptan has high affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower with a pEC50 value of 8.2 for the 5-HT1B receptor, compared to a pEC50 value of 6.2 for the 5-HT7 receptor.
L3169 LP 12 hydrochloride hydrate ≥98% (HPLC), solid LP 12 dihydrochloride is a 5-HT7 receptor agonist displaying selectivity over D2, 5-HT1A and 5-HT2A receptors (Ki values are 0.13, 224, 60.9 and 1464 nM, respectively. It also displays selectivity over D2, 1723; over 5-HT1A, 468; over 5-HT2A, 11261; and high potency. Sigma has added LP 44 (L9793) which shows significantly lower D2 selectivity (7.3 nM/0.22 nM for 33-fold), lower selectivity over 5-HT1A, 240; and over 5-HT2A, 1482. LP 12 and LP 44 seem to share a common intermediate.
SML1561 LP-211 ≥98% (HPLC) LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor. The 5-HT7 receptor is involved in a variety of central nervous system functions including circadian rhythm, sleep, thermoregulation, nociception, and memory, and appears to be involved in cognitive disorders, anxiety, and depression. LP-211 has been used as a selective 5-HT7 receptor agonist in multiple models including studies as a potential therapeutic agent in models of Rett syndrome and Fragile X Syndrome.
L9793 LP44 ≥98% (HPLC), solid LP44 is a high affinity 5-HT7 receptor agonist. Ki = 0.22 nM. LP44 displays selectivity over 5-HT1A and 5-HT2A receptors (200- and >1000-fold, respectively). LP44 induces relaxation of substance P-stimulated guinea pig ileum (EC50 = 2.56 μM).
S009 LY-165,163 solid Selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.
SML0010 LY-334370 hydrochloride hydrate ≥98% (HPLC), powder LY-334370 hydrochloride is a selective 5-HT1F receptor agonist.
LY-334370 modulates the transmission in the mouse trigeminal system and inhibits the neuronal responses within rat Sp5C by inhibiting c-Fos activation. It shows efficacy in aborting migraine attacks.
SML0556   LY344864 hydrochloride ≥98% (HPLC) LY344864 hydrochloride is a potent and selective 5-HT1F receptor agonist. It has an EC50 of 3 nM, and displays > 80-fold selectivity over other 5-HT receptors
SML1038 MKC-733 ≥98% (HPLC) MKC-733 is a 5-HT3 specific agonist.
M7319 ML 10302 ≥98%, solid Potent, selective 5-HT4 serotonin receptor agonist
M2946 Mosapride citrate salt dihydrate 5-HT4 receptor agonist and 5-HT3 receptor antagonist
Q107 N-Methylquipazine dimaleate salt solid Tertiary amine analog of quipazine that is an agonist at 5-HT3 serotonin receptors with an affinity similar to that of quipazine, but which lacks affinity for central 5-HT1B serotonin receptors.
N1415 Naratriptan hydrochloride ≥98% (HPLC) Naratriptan hydrochloride is a serotonin 5-HT1B/1D receptor agonist.
SML1255 Nonyloxytryptamine oxalate ≥98% (HPLC) Nonyloxytryptamine (5-nonyloxytryptamine) is a potent and selective 5-HT1B receptor agonist. Nonyloxytryptamine is a polysialic acid (PSA) mimick that triggers PSA-mediated functions. Nonyloxytryptamine enhances neurite outgrowth of cultured primary neurons, protects neurons from oxidative stress, enhanced Schwann cell proliferation, reduces migration of astrocytes and enhances myelination in vitro.
M6628 O-Methylserotonin hydrochloride crystalline Nonselective serotonin receptor agonist that lacks affinity for the 5-HT3 receptor.
PZ0229 PF-03246799 hydrochloride ≥98% (HPLC) PF-3246799 is a potent serotonin 5-HT2C receptor agonist with an EC50 of 4.5 nM and minimal activity at 5-HT2A and 5-HT2B receptors. PF-3246799 had good efficacy in a preclinical canine model of stress urinary incontinence.
PZ0032 PF-04479745 ≥98% (HPLC) PF-04479745 (PF-4479745) is a selective serotonin 5HT2C agonist.
PZ0310 PF-04995274 ≥98% (HPLC) PF-04995274 is a potent partial agonist of serotonin 5HT4 receptor with Ki = 0.15 - 0.46 nM for 5-HT4 isoforms a, b, d and e. 5-HT4 agonists modulate cholinergic function are being studied as possible treatment for cognitive disorders associated with Alzheimer′s Disease. PF-04995274 is brain penetrant and was shown to increase brain acetylcholine levels and reversed scopolamine-induced learning deficits in the rat Morris water maze test.
SML1371 Prucalopride ≥98% (HPLC) Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activity. 5-HT4 receptors are GPCRs that are expressed in the CNS and peripheral tissues. The receptor has a role in GI motility disorders such as irritable bowel syndrome and idiopathic constipation. Agonists are prokinetic and of potential use for disoroders of reduced motility. Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activities. Prucalopride has pK(i) values of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively, and at least 290-fold selectivity for 5-HT4 over other serotonin and dopamine receptors.
Q1004 Quipazine maleate salt Non-selective serotonin receptor agonist.
U109 R(+)-UH-301 hydrochloride solid R(+)-UH-301 hydrochloride is a potent and selective 5-HT1A serotonin receptor agonist. R(+)-UH-301 is also known to function as an antinociceptive agent, as it has been shown to significantly decrease formalin-induced flinching in rats.
SML0247 Rizatriptan benzoate salt ≥98% (HPLC) Rizatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine.
H141 S(−)-8-Hydroxy-DPAT hydrobromide solid Partial 5-HT1A serotonin receptor agonist.
D154 S(+)-DOI hydrochloride solid Less potent enantiomer of (±)-DOI.
S5321 S15535 ≥98% (HPLC), solid Potent, orally active, partial 5-HT1A receptor agonist
S15535, a benzodioxane, is a selective but partial agonist of histamine 5-HT1A receptor. It activates presynaptic 5-HT1A receptors and suppresses the release of hippocampal 5-HT. It acts as anxiolytic agent and modulates the cholinergic and cognitive function in rodents.3,4
PZ0146 SC-53116 hydrochloride hydrate ≥98% (HPLC) SC-53116 is a 5-HT4 receptor partial agonist. SC-53116 has been shown to ameliorate scopolamine-induced impairment in learning in rats at a does of 10 μg/rat i.c.v and increase population spike amplitude in the CA1 and CA3 fields of the hippocampus at the same concentration.
S1688 SR 57227A solid Potent and selective 5-HT3 serotonin receptor agonist.
SR 57227A is a highly selective of central and peripheral 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreased isolation-induced aggressive behavior.
SML0260 ST1936 ≥98% (HPLC) ST1936 is a high affinity 5-HT6-specific agonist (Ki = 13 nM). The IC50 for competition of LSD from 5-HT6 expressed in HEK cells is 40 nM, and the EC50 for stimulating cAMP production is 16 nM.
H7752 Serotonin creatinine sulfate monohydrate powder Neurotransmitter.
H9523 Serotonin hydrochloride powder Neurotransmitter.
H4511 Serotonin hydrogen maleate powder Neurotransmitter.
H7877 Serotonin hydrogenoxalate powder Neurotransmitter.
S6319 Sertraline hydrochloride ≥98% (HPLC) Selective serotonin reuptake inhibitor, antidepressant.
Sertraline suppresses platelet function and exhibits antiplatelet and endothelium protective functions. It relieves depression and improves the quality of life in patients with cardiovascular disorders. It can also be prescribed to treat depression in Parkinson′s disease.
S1198 Sumatriptan succinate ≥98% (HPLC), solid Sumatriptan succinate is a 5-HT1 serotonin receptor agonist.
PZ0279   Sunepitron hydrochloride Sunepitron hydrochloride is a combined serotonin 5-HT1A receptor agonist and α2-adrenergic receptor antagonist. Sunepitron hydrochloride has been tested for the treatment of depression and anxiety.
SML1698 TMPPAA ≥98% (HPLC) TMPPAA is an allosteric agonist and positive allosteric modulator (PAM) of 5-HT3 receptor. TMPPAA behaves as both an agonist and a PAM at 5-HT3A receptors, not via binding at the orthosteric site.
T6704 Tandospirone ≥98% (HPLC) Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. The potency of tandospirone is equal to that of buspirone and approximate half that of diazepam. The potency of tandospirone as a dopamine antagonistic is less than 1/4 that of buspirone.
SML1504 Tegaserod maleate ≥98% (HPLC) Tegaserod is a potent full agonist at serotonin 5-HT4 receptors with an EC50 of 7 nM.
PZ0305 WAY-208466 dihydrochloride ≥98% (HPLC) WAY-208466 is a high affinity (Ki = 4.8 nM) 5-HT6 receptor agonist. In HeLa cells expressing cloned human 5-HT6, the compound induced cAMP production (EC50 = 7.3 nM; Emax = 100%). WAY-208466 increases cortical GABA levels and exhibits anxiolytic activity in rat studies.
X4879 Xaliproden hydrochloride ≥97% (HPLC), solid 5-HT1A serotonin receptor agonist; neuroprotectant
SML0248 Zolmitriptan ≥98% (HPLC) Zolmitriptan is a selective serotonin receptor agonist of the 5HT1B and 5HT1D subtypes, both centrally and peripherally. It has been used clinically for the acute treatment of migraine attacks with or without aura and cluster headaches.
M110 α-Methylserotonin maleate salt ≥98% (HPLC) 5-HT2 serotonin receptor agonist.
U6883 cis-Urocanic acid ≥98% (HPLC), solid (fluffy) cis-Urocanic acid, a 5-HT agonist, is a product of uv isomerization of trans-urocanic acid in skin, which leads to immunosuppression via activation of 5-HT2A receptor.