5-HT Receptor Agonist

CP94253 is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 can be used for the research of depression and heightened aggressive behavior.

Avitriptan is a 5-HT_1B/1D receptor agonist, with pK_is of 7.44 ( 5-HT_1B rat), 7.68 ( 5-HT_1B human) and 8.36 ( 5-HT_1D human). Avitriptan constricts the isolated coronary artery. Avitriptan can be used for migraines.

Osemozotan hydrochloride (MKC242) is a selective 5-HT_1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder.

VU6067416 is a potent and brain-penetrant 5-HT2A agonist with an EC₅₀ of 189 nM.

Urapidil-d₄ is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

CP 93129 is a potent and selective 5-HT_1B agonist. CP 93129 has the potential for the research of Parkinson's disease.

Quetiapine sulfone is a main metabolite of Quetiapine (HY-14544). Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.

Capeserod hydrochloride (SL65.0155) is a 5-HT_4(e) receptor partial agonist (K_i=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT_4(b) and 5-HT_4(e) splice variants, stimulating cAMP production with IC₅₀ values of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia.

PF-04781340 is a potent and selective 5-HT₂C receptor agonist, with an EC₅₀ of 9 nM and a K_i of 3 nM, respectively. PF-04781340 exhibits weak partial agonist activity at the 5-HT₂B receptor, with an EC₅₀ of 1484 nM. PF-04781340 can be used in the research of obesity and psychiatric disorders.

5-HT2A receptor agonist-9 (Compound 9) is a β-arrestin-biased 5-HT_2A receptor agonist. 5-HT2A receptor agonist-9 can be used in the research of neurological diseases such as antidepressant and psychedelic.

Tiflucarbine (BAY-P 4495) is a tetrahydrothieno-7-carboline derivative. Tiflucarbine is a potent antidepressant agent that binds at central serotonin (5-HT) binding sites. Tiflucarbine is a nonselective 5-HT (5-HT1 and 5-HT2) agonist.

5-HT2A agonist 7 (Compound 45) is an orally active and highly selective serotonin receptor 2A (5-HT_2A) agonist (EC₅₀=12 nM). 5-HT2A agonist 7 is promising for research of psychiatric disorders such as depression.

Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

Rizatriptan (MK 462) hemisulfate hemihydrate is the agonist for 5-HT_1B and 5-HT_1D. Rizatriptan hemisulfate hemihydrate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system.

Cisapride-d₆ (R51619-d₆) is the deuterated-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

2C-TFM hydrochloride is a ,5-dimethoxyphenethylamines compound with a para-trifluoromethyl substitution. 2C-TFM hydrochloride is a potent agonist of the 5-HT receptor subtypes 5-HT2A and 5-HT2C.

THRX-194556 is a 5-HT₄ receptor agonist. THRX-194556 can be used to study gastrointestinal functional disorders and Alzheimer’s disease.

5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT_2CR partial agonist (E_max=71.09%) with an EC₅₀ value of 121.5 nM and no observed activity toward 5-HT_2AR or 5-HT_2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM.

Zolmitriptan-d₆ is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.

Sumatriptan-d₅ is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research.