rat 5-ht7 receptor

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist with pKis of 8.19 and 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.

LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

Repinotan (BAY x 3702 free base) is an orally active, selective 5-HT1A receptor agonist that crosses the blood-brain barrier (BBB), exhibits neuroprotective activity, counteracts morphine-induced depression of ventilation in anesthetized rats, and may be used in studies of acute ischemic stroke and traumatic brain injury.

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

AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).

5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active compound capable of crossing the blood-brain barrier, serving as a ligand for both 5-HT7 and 5-HT2A receptors with a pKi of 8.1 at each receptor. It acts as an antagonist in vitro in 5-HT2A functional assays and as an inverse agonist in 5-HT7 functional assays. This compound blocks hypothermia in rats induced by 5-Carboxamidotryptamine (5-CT) and prevents head twitches in mice caused by 2,5-Dimethoxy-4-iodoamphetamine (DOI). Additionally, it occupies 5-HT2A receptor binding sites in the frontal cortex of rat brains and is applicable in the study of neurological disorders.

PZ-1657 hydrochloride (Compound 57) is a potent, selective, and orally active 5-HT7 receptor inverse agonist, with a Ki value of 5 nM. It inhibits constitutive cAMP production mediated by the Gs signaling pathway, with an EC50 value of 2.93 nM. PZ-1657 hydrochloride significantly reduces 5-HT7 receptor-mediated MMP-9 activity in the mouse hippocampus, showing effects comparable to SB-269970. It reverses cognitive deficits induced by phencyclidine in a rat novel object recognition test without affecting spontaneous activity. PZ-1657 hydrochloride is useful for researching affective disorders such as depression and bipolar disorder.

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1/2 and Fyn kinase.

LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.