5-ht1 receptor

NEO 376 (SPI-376) is a selective 5-HT1 receptor, GABA receptor and dopamine receptor modulator, showing anti-psychotic actively.

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Rodatristat ethyl (KAR5585) is a groundbreaking, orally active, and potent inhibitor of tryptophan hydroxylase 1 (TPH1) that significantly reduces 5-hydroxytryptamine (5-HT) levels and decreases pulmonary arterial hypertension (PAH) at low concentrations.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Perospirone hydrochloride (Perospirone HCl) is an atypical antipsychotic agent for the treatment of schizophrenia. It also displays affinity towards 5HT1A receptors as a partial agonist.

Cinanserin is a serotonin 5-HT2 antagonist.

Sumatriptan succinate (GR 43175), a serotonin1 (5-HT1) receptor agonist, is used in the acute treatment of a migraine headache.

Sumatriptan (GR 43175 free base) is an orally active and potent 5-hydroxytryptamine 1 (5-HT1) receptor agonist that crosses the blood-brain barrier and has anti-inflammatory activity with high affinity for 5-HT1D, 5-HT1B, and 5-HT1F receptors for use in acute migraines and acute myocardial infarction.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.

Naratriptan D3 Hydrochloride, the deuterium-labeled form of Naratriptan, is a selective agonist of the 5-HT1 receptor subtype.

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

Dehydro Palonosetron (RS 42358-197) is a potent, selective, and orally active 5-HT3 receptor antagonist. It does not affect the activity of 5-HT1 receptors, 5-HT2 receptors, or 5-HT4 receptors.

Cinitapride (Blaston) is a gastroprokinetic agent. It slows the actions of the muscles to reduce the symptoms of conditions such as acid reflux, delayed gastric emptying, and ulcer dyspepsia. Cinitapride acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors.

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors

5-Carboxamidotryptamine maleate (5-CT maleate) is a receptor agonist with antihypertensive and glucose-raising effects.

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

Metergoline (Methergoline) is a dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for migraine disorder therapy.

Methiothepin maleate (Metitepine) is a 5-HT1, 5-HT6, 5-HT7 serotonin receptor antagonist, which blocks serotonin autoreceptors.

Sumatriptan (GR 43175) hydrochloride can be used in the research of migraine headache that is an orally active agonist of 5-HT1 receptor. The Ki values of Sumatriptan hydrochloride against 5-HT1D, 5-HT1B and 5-HT1A receptors are 17 nM, 27 nM and 100 nM, respectively. [1] [2].

Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride (GR-85548A hydrochloride) binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.

Isamoltane is a serotonin 5-HT1 Receptor Antagonist

Avitriptan, also known as BMS-180048, is a selective 5-HT1-like receptor agonist. Avitriptan is an effective compound for the treatment of migraine headaches with a prolonged duration of response. Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.

Naratriptan is a selective agonist of 5-HT1 receptor and is is used for the treatment of migraine headaches.