serotonin receptor

BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

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

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.

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

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.

Rotundine (Gindarine) (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.

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.

Brexpiprazole HCl (OPC 34712 dihydrochloride) is a new antipsychotic drug.

Quetiapine hemifumarate (ICI-204636), an atypical antipsychotic, is used in the treatment of bipolar I mania, schizophrenia, bipolar II depression, bipolar I depression.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural compound derived from the roots and rhizomes of Notopterygium incisum.

Urapidil hydrochloride (Urapidil HCl) is 5-HT1A receptor agonist and an α1-adrenoceptor antagonist.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

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

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

Cyproheptadine hydrochloride (Periactin hydrochloride) is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.

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

Serotonin (5-hydroxytryptamine) is a natural product from animals

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.