5-ht2

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

Adatanserin hydrochloride (WY50324 hydrochloride) is a novel 5-HT(1A)/5-HT(2) receptor ligand with potential neuroprotective effects and inhibition of ischemic efflux of endogenous amino acids, which can be used in the study of depression and anxiety disorders.

Tiospirone (BMY 13859-1 free base) is a 5-HT2 receptor antagonist and dopamine blocker that inhibits D2, 5-HT1a, 5-HT7, and sigma receptors.Tiospirone is used in the study of neurological disorders such as schizophrenia.

BF-1 is a novel selective 5-HT2 receptor antagonist that acts by blocking neurogenic dural plasma protein extravasation induced by mCPP or BW723C86.BF-1 is used in the study of migraine.

Aplindore Fumarate (DAB-452) is a small molecule dopamine D2 receptor partial agonist.Aplindore Fumarate exhibits high affinity for dopamine D2 and D3 receptors, and low affinity for dopamine D4, 5-hydroxytryptophan (5-HT2), and α1-adrenergic receptors.Aplindore Fumarate is used in the study of Parkinson's disease and schizophrenia. Fumarate can be used to study Parkinson's and schizophrenia.

Gevotroline, a chemical in palm wine that can be used to treat psychosis, is a 5-HT2 receptor antagonist that can be used to study behavioral disorders.

Serazapine is a highly specific serotonin (5-HT2) binding inhibitor with anxiolytic activity for the treatment of anxiety disorders.

CI 169369 is a selective 5-HT2 receptor antagonist used in the study of anxiety and depression.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

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

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

AMI-193 (Spiramide) is an effective and selective antagonist of 5-HT2 and D2 receptor with Kis of 2, 3, 50, 2530, and 4300 nM for 5-HT2, D2 Receptor, 5-HT1A, D1 Receptor, and 5-HT1C Receptor. AMI-193 shows antipsychotic activity.

Cyproheptadine hydrochloride sesquihydrate (Peritol), an antihistamine, is an antagonist of serotonin and histamine2.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

(S)-Mirtazapine ((S)-Org3770) is the S(+)-enantiomer of Mirtazapine, functioning as a selective 5-HT2 receptor antagonist with pro-nociceptive effects. It is commonly used in combination with the R(-)-enantiomer of Mirtazapine to study depression.

Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).

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.

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.