BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist.
BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist. Serotonin (5-HT) is a major neurotransmitter that acts through a family of GPCRs and one ion channel. 5-HT4 receptor is GPCR expressed in many tissues, including brain, and modulates dopamine secretion, learning, and memory. BIMU8 is a full agonist at 5-HT4, but it binds differently than the endogenous ligand, 5-HT, shown through site-directed mutagenesis studies. It depolarizes neurons and was used to localize 5-HT4 to somatic but not dendritic regions of CA1 pyramidal neurons.
5-HT₄ receptor (5-HT₄R) activation induces procognitive effects. This might be related to stimulation of hippocampal acetylcholine release, which has been shown for 5-HT₄R agonists in in-vivo models. We investigated the influence of the 5-HT₄R agonists, prucalopride and BIMU-8, on acetylcholine
The Journal of pharmacology and experimental therapeutics, 286(3), 1115-1121 (1998-09-11)
The effects of the administration of different 5-HT4 receptor antagonists (SDZ 205557, GR 125487) and 5-HT4 receptor agonists (BIMU 1, BIMU 8) on memory processes were evaluated in the mouse passive avoidance test. The administration of SDZ 205557 (10 mg
Serotonin (5-HT) is involved in a large variety of physiological functions and it appears now that it could play a role in cognitive processes through the activation of 5-HT4 receptors. The present study was conducted to determine the effect of
Pharmacology, biochemistry, and behavior, 56(3), 347-351 (1997-03-01)
In the present work, the effects of pre- or post-training (ip) injection of BIMU1 and BIMU8 (5-HT4 agonists) were figured out in the autoshaping learning task. Furthermore, the post-training effects of these agonists after treatment with SDZ 205-557 and GR
Recently, a 5-hydroxytryptamine (5-HT) receptor has been described, whose pharmacology was distinct from that of the already known serotonergic receptors, so that it has been called 5-HT4. Because the lack of a high affinity radioligand, the identification of this receptor
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