Serotonergics - Agonists

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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.
human ... HTR1E(3354), HTR1F(3355)
B7148 Buspirone hydrochloride 5-HT1A serotonin receptor agonist; anxiolytic.
human ... HTR1A(3350)
B175 BW 723C86 ≥98% (HPLC) 5-HT2B serotonin receptor agonist.
human ... HTR2B(3357)
C117 5-Carboxamidotryptamine maleate salt powder, ≥98% (HPLC) Agonist at 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 serotonin receptors.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR2A(3356), HTR2C(3358), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
rat ... Htr7(65032)
C106 CGS-12066 maleate salt solid 5-HT1B serotonin receptor agonist.
human ... HTR1B(3351)
C144 1-(3-Chlorophenyl)biguanide hydrochloride solid Very potent 5-HT3 serotonin receptor agonist.
human ... HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
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.
 
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.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
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.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
PZ0011 Eletriptan hydrobromide ≥98% (HPLC) Eletriptan hydrobromide is a serotonin 5-HT1B/1D receptor agonist; second generation anti-migraine drug.
 
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.
 
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.
 
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.
human ... HTR1A(3350), HTR1D(3352)
M110 α-Methylserotonin maleate salt ≥98% (HPLC) 5-HT2 serotonin receptor agonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
M6628 O-Methylserotonin hydrochloride crystalline Nonselective serotonin receptor agonist that lacks affinity for the 5-HT3 receptor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
M7319 ML 10302 ≥98%, solid Potent, selective 5-HT4 serotonin receptor agonist
rat ... Htr3a(79246), Htr4(25324)
M2946 Mosapride citrate salt dihydrate 5-HT4 receptor agonist and 5-HT3 receptor antagonist
 
N1415 Naratriptan hydrochloride ≥98% (HPLC) Naratriptan hydrochloride is a serotonin 5-HT1B/1D receptor agonist.
 
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.
 
Q1004 Quipazine maleate salt Non-selective serotonin receptor agonist.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
SML0247 Rizatriptan benzoate salt ≥98% (HPLC) Rizatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine.
 
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.
 
H7752 Serotonin creatinine sulfate monohydrate powder Neurotransmitter.
human ... HTR3A(3359)
H9523 Serotonin hydrochloride powder Neurotransmitter.
human ... HTR3A(3359)
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.
human ... HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
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.
 
S1198 Sumatriptan succinate ≥98% (HPLC), solid Sumatriptan succinate is a 5-HT1 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.
human ... HTR1A(3350)
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.