5-HT Receptor

Brilaroxazine (RP5063): multimodal dopamine/5-HT modulator, partial agonist at D2/D3/D4, 5-HT1A/2A, and antagonist at 5-HT2B/7.

Bexicaserin (Compound 3), a 5-HT2C receptor agonist, has potential applications in research pertaining to obesity and psychiatric disorders [1].

13,14-dihydro-15-keto Prostaglandin E2 (13,14-dihydro-15-keto PGE2) serves as the predominant metabolite of PGE2 in plasma, created through a 15-keto PGE2 intermediate by the action of 15-oxo-PG Δ13 reductase. Unlike its precursor PGE2, this compound exhibits poor binding affinity towards EP2 and EP4 PGE2 receptors (Ki values of 12 and 57 µM, respectively) in CHO cells and fails to stimulate adenylate cyclase activity therein (EC50s >18 and >38 µM, respectively). Concentrations of 13,14-dihydro-15-keto PGE2 are notably higher in the plasma of pregnant women during their third trimester and at labor and delivery stages, whereas its levels are found to be reduced in the tumor tissues of patients with non-small cell lung cancer (NSCLC) compared to adjacent healthy tissue.

Amesergide is an orally active and selective serotonin (5-HT1/2) antagonist that inhibits weight gain in offspring of female CD rats, for depression research.

PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.

SB 258719 is a selective antagonist of 5-HT7 receptor with pKi of 7.5.

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM.

R-96544 is an orally active antagonist of the 5-HT2A receptor that has demonstrated the ability to inhibit platelet aggregation in vitro [1].

5-HT3 antagonist 1 is a potent and selective antagonist of 5-HT3 receptor.

L-772,405 is a highly selective agonists of h5-HT(1D) receptor.

SB 649915 is a serotonin reuptake inhibitor and 5-HT1A and 5-HT1B receptor antagonist.

Velusetrag(TD-5108), a potent 5-HT4 agonist, is in development for gastroparesis, constipation, and IBS.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

Selective, high affinity 5-HT1A receptor antagonist

GR 125487 sulfamate is a 5-HT4 receptor antagonist.

Flesinoxan HCl is the salt form of Flesinoxan, which is a selective 5-HT1A receptor agonist.

NAS-181 free base is a 5-HT(1B) receptor antagonist.

(S)-Renzapride (BRL 24924), 5-HT4 agonist (Ki 115 nM), 5HT2b/5HT3 antagonist, for C-IBS study.

UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM).

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

5-HT1B/1D receptor antagonist

1-Carboxycyclohexaneacetic acid may be present as a potential impurity in commercial gabapentin, an antiepileptic drug. Furthermore, it serves as a precursor for synthesizing antagonists targeting the serotonin (5-HT) receptor subtype 5-HT2A.

Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant

MDL-74156 is an active metabolite of dolasetron and a 5-hydroxy-tryptamine3 (5-HT3) antagonist.

Butriptyline (Butriptylene), a tricyclic antidepressant, is effective when administered orally [1].

Abaperidone is an atypical antipsychotic, antagonizes 5-HT2A (IC50=6.2 nM) and D2 receptors (IC50=17 nM), reduces hsp70 mRNA in rat brains.

Indeloxazine HCl: Serotonin releaser, NE reuptake inhibitor, NMDA antagonist; antidepressant that boosts acetylcholine in rats.

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.

5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC 50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced

Compound 24 (5-HT2 agonist-1 free base) is a potent agonist for 5-HT2A, 5-HT2B, and 5-HT2C receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM,

4-Chloro-L-phenalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis and a non-specific antagonist of tryptophan hydroxylases (TPH1 and TPH2).

LY320954 is an antagonist of 5-HT2A receptor.

YM348 is an effective and orally active 5-HT2C receptor agonist. YM348 also shows a high affinity for the cloned human 5-HT2C receptor (Ki: 0.89 nM).

GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist.

Frovatriptan, potent 5-HT 1B/D agonist, shows high cerebroselectivity and efficacy for migraine with aura.

Robalzotan is a selective 5-HT1A receptor antagonist.

rat 5-HT1B receptor antagonist

Osemozotan Free Base is a 5-HT(1A) receptor agonist.

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively.

CP-122288: potent, selective 5-HT1B/D/F agonist; inhibits plasma protein extravasation, neurogenic inflammation.

MIN-117, a SSRI/5-HT receptor antagonist, is potentially used for the treatment of depression.

5-HT2A&5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting the 5-HT2A and 5-HT2C receptors with respective IC50 values of 196 nM and 0.9 nM.

Nemonapride is a dopamine D2-like receptor antagonist.

5-HT3-In-1 (compound example 8) exhabits with 5-HT3 inhibition activity.

(S)-Bexcaserin (compound 2) serves as a 5-HT2C receptor agonist, presenting research possibilities in obesity and psychiatric disorders [1].

SB 216641 hydrochloride (SB-216641A) is a 5-HT1B/D receptor antagonist with anxiolytic properties.

WAY-607695 is a potential 5-HT1A receptor agonist.

Didesmethyl cariprazine, Cariprazine's active metabolite, treats schizophrenia/bipolar with D3/D2 affinity; half-life 1-3 weeks.

Osemozotan is a 5-HT1A receptor agonist potentially for the treatment of generalized anxiety disorder.