5-HT Receptor Agonist

5-HT2A receptor agonist-3 ((S,S)-9b) is a 5-HT2A receptor agonist with a K_i of 2.5 nM for human 5-HT2A receptor. 5-HT2A receptor agonist-3 shows 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.

5-HT2A receptor agonist-1 (Compound 3) is a selective 5-HT2A receptor agonist with the EC₅₀ of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders.

Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT_1A receptor agonist (K_i=0.19 nM). Hypidone hydrochloride inhibits the uptake of [³H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC₅₀s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.

Tandospirone (SM-3997) citrate is a potent and selective 5-HT_1A receptor partial agonist, with a K_i of 27 nM. Tandospirone citrate has anxiolytic and antidepressant activities. Tandospirone citrate can be used for the research of the central nervous system disorders and the underlying mechanisms.

IHCH-7113 is a 5-HT2AR agonist with EC₅₀ values of 58.9 nM (Gq bioluminescence resonance energy transfer assay) and 44.7 nM (β-arrestin 2 bioluminescence resonance energy transfer assay). IHCH-7113 activates both Gαq-mediated signaling pathways and β-arrestin 2 recruitment pathways. IHCH-7113 is applicable for research related to depression.

Serotonin (5-Hydroxytryptamine) (Standard) hydrochloride is the analytical standard of Serotonin hydrochloride (HY-B1473). This product is intended for research and analytical applications. Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

5-Hydroxytryptamine creatinine sulfate monohydrate is a 5-HT receptor agonist and amine oxidase substrate that acts through multiple physiological responses, including induction of vasoconstriction, pressor effects, acceleration of platelet potassium exchange, and endothelium-dependent relaxation, and can serve as a radiolabeled substrate for organelle uptake assays. 5-Hydroxytryptamine creatinine sulfate monohydrate can be used in research on burns, tourniquet and botulinum shock.

Ro60-0175 is a potent and selective agonist of 5-HT_2C receptor. Ro60-0175 reduces self-administration.

MK-212 monohydrochloride (CPP monohydrochloride) is an orally active, blood-brain barrier permeable agonist of 5-HT₁C, 5-HT₂ and 5-HT₁A receptors. MK-212 monohydrochloride induces hyperthermia, nausea, arousal, irritability and restlessness, inhibits the elevation of plasma cortisol and prolactin, and reduces feelings of calmness and overall positive affect. MK-212 monohydrochloride mediates anxiety-like behaviors and motor inhibition. MK-212 monohydrochloride is applicable to research related to schizophrenia and anxiety disorders.

5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action.

GR-46611 is a 5-HT_1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia.

Nemonapride is a highly potent dopamine D₂ receptor antagonist with a K_i of 0.06 nM. Nemonapride also activates 5-HT_1A receptor with an IC₅₀ of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals.

Donitriptan is a potent, high efficacy agonist at 5-HT_1B/1D receptors with pK_is of 9.4 and 9.3, respectively.

Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice.

Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT4R), with a pK_i of 7.7. Velusetrag exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease.

F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.

Almotriptan (PNU180638 free base) 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 shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine.

SB 206553 is a 5-HT_2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT_2A), 7.7 nM (5-HT_2B) and 7.8 nM (5-HT_2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders.

Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABA_A receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.

α-Methylserotonin maleate is a potent and selective agonist of 5-HT₂ receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis.