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Pergolide acts as an agonist of dopamine D 2 and D 1 and serotonin 5-HT 1A, 5-HT 1B, 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors.It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline.
F-15,063 is an orally active potential antipsychotic, and an antagonist at the D 2 /D 3 receptors, partial agonist at the D 4 receptor, and agonist at the 5-HT 1A receptors. It has greater efficacy at the 5-HT 1A receptors than other antipsychotics, such as clozapine, aripiprazole, and ziprasidone.
WAY-100635 is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a selective 5-HT 1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D 4 receptor.
F-15,599, also known as NLX-101, is a potent and selective 5-HT 1A receptor full agonist. [1] [2] In addition, it displays functional selectivity, or biased agonism, by preferentially activating postsynaptic serotonin 5-HT 1A receptors over somatodendritic serotonin 5-HT 1A autoreceptors.
Likewise, 4-F-5-MeO-pyr-T does not substitute for the psychedelics DOI and LSD in animal drug discrimination tests. [3] However, it fully substitutes for the serotonin 5-HT 1A receptor full agonist LY-293284 in such tests. [3] 4-F-5-MeO-pyr-T produces serotonin 5-HT 1A receptor-dependent antidepressant-like effects in rodents. [4] [5] It also ...
L-694247 is a somewhat selective 5-HT 1D agonist, with a 10-fold greater affinity for the 5-HT 1B receptor, and 25-fold greater affinity for the 5-HT 1A receptor. [1] When L-694247 was injected intraventricularly in dehydrated rats, it inhibited water intake. Pre-treatment with a 5-HT 1D antagonist abolished this effect. Administration of L ...
LY-334370 is a selective 5-HT 1F receptor agonist [1] which was under development by Eli Lilly and Company for the treatment of migraine headaches. [2] The drug showed efficacy in a phase II clinical trial [ 3 ] but further development was halted due to toxicity detected in animals.
The selectivity and affinity of ergolines for certain 5-HT receptors can be improved by introducing a bulky group on the phenyl ring of the ergoline skeleton, which would prevent the interaction of ergoline derivatives with receptors. [30] This methodology has been used to develop selective 5-HT 1A and 5-HT 2A ergolines in particular.