5-HT Receptor Inhibitor

5-IAI hydrochloride is a psychoactive analog of p-iodoamphetamine and is indistinguishable, in its physiological effects. 5-IAI hydrochloride significantly reduces both serotonin uptake sites and hippocampal serotonin levels in rats.

Paroxetine (BRL29060) acetate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine acetate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine acetate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine acetate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

Cyproheptadine (Standard) is the analytical standard of Cyproheptadine (HY-B1622). This product is intended for research and analytical applications. Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats.

Paroxetine-d₄ (BRL29060-d₄) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

PCPA methyl ester (hydrochloride) (Standard) is the analytical standard of PCPA methyl ester (hydrochloride) (HY-101456). This product is intended for research and analytical applications. PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.

PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research.

ARC 239 (Standard) is the analytical standard of ARC 239. This product is intended for research and analytical applications. ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM.

Carboetomidate is a pyrrole derivative analogous to the sedative-hypnotic drug Etomidate, which induces general anesthesia while avoiding the inhibition of adrenal steroid synthesis. Carboetomidate enhances GABA_A receptor function via β2/β3 subunits, inhibits neuronal nicotinic acetylcholine receptors (nAChR) and 5-HT₃A receptors, and increases plasma IL-10 levels during endotoxemia. Carboetomidate is applicable to research related to sepsis and sleep disorders.

(R)-Viloxazine-d₅ hydrochloride ((R)-Viloxazin-d₅ hydrochloride; (R)-Emovit-d₅ hydrochloride) is the deuterated-labeled (R)-Viloxazine hydrochloride (HY-125784A). (R)-Viloxazine hydrochloride is the less active R-isomer of Viloxazine hydrochloride (HY-125784). (R)-Viloxazine hydrochloride can be used in the research of depression.

Diclofensine (Ro 8-4650) hydrochloride (Standard) is the analytical standard of Diclofensine hydrochloride. This product is intended for research and analytical applications. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.

LY266097 hydrochloride (Standard) is the analytical standard of LY266097 hydrochloride (HY-103094). This product is intended for research and analytical applications. LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pK_is of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.

Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1).

Nefazodone (Standard) is the analytical standard of Nefazodone. This product is intended for research and analytical applications. Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.

18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC₅₀ values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine also exhibits potent antiparasitic activity. 18-Methoxycoronaridine can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis.

Teniloxazine is an inhibitor for norepinephrine neuronal reuptake and an weak inhibitor for reuptake of Serotonin (HY-B1473A) and Dopamine (HY-B0451). Teniloxazine exhibits antidepressant, antihypoxic and anti-amnestic properties without anticholinergic, sedative, and cardiovascular adverse effects.

Cloroperone is a 5-HT₂ receptor inhibitor with a K_i value of 4.5 nM. Cloroperone can be used in research on psychiatric disorders.

Alaproclate is an inhibitor for serotonin (5-HT) reuptake. Alaproclate affects mechanisms that related to cued navigation performance such as sensory, sensorimotor, or motivational factors, impairs spatial navigation ability of rats.

Antidepressant agent 10 (Standard) is the analytical standard of Antidepressant agent 10 (HY-W009754). This product is intended for research and analytical applications. Antidepressant agent 10 is an orally active antidepressant compound that inhibits the serotonin 5-HT1A and 5-HT2 receptors, with corresponding IC₅₀ values of 190 nM and 110 nM, respectively.

Pirandamine free base is a selective serotonin (5-HT) (HY-B1473A) uptake inhibitor with an IC₅₀ of 250 nM. It exerts antidepressant-like effects by enhancing central serotonergic function, does not inhibit norepinephrine (HY-13715) uptake, and exhibits no central anticholinergic or monoamine oxidase inhibitory activity. Pirandamine free base is used in the study of depression.