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SB-216641 and BRL-15572 – compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors
TLDR
Both compounds were partial agonists in these high receptor expression systems, with potencies and selectivities which correlated with their receptor binding affinities, and will be useful pharmacological agents to characterise 5- HT1B and 5-HT1D receptor mediated responses. Expand
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine]
TLDR
This paper describes how, using computational chemistry models as a guide, the nonselective 5- HT1B/5-HT1D receptor antagonist 4 was structurally modified to produce the selective 5-HT 1B receptor inverse agonist 5. Expand
Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding
TLDR
Direct evidence for the existence of 5-HT3 receptors in rat brain tissue and their distribution is reported, based on high affinity binding of the potent 5- HT3 receptor antagonist 3H-GR65630 to homogenates of rat entorhinal cortex. Expand
Behavioural and biochemical consequences following activation of 5HT1-like and GABA receptors in the dorsal raphé nucleus of the rat
TLDR
These findings, together with available electrophysiological data suggest that these behavioural responses are a consequence of a depression of the firing of cells in the dorsal raphé nucleus, with a corresponding decrease in functional activity of 5-HT in the forebrain. Expand
The medical benefit of 5-HT research
TLDR
The role of 5-HT in the mechanism of action of antipsychotic agents remains a topic of intense research, which promises better treatments for schizophrenia in the future. Expand
5‐HT3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis in the ferret
TLDR
Results confirm a role of 5‐HT, and in particular 5‐ HT3 receptors, in the control of cisplatin‐induced emesis, and show that at least one functional site for these receptors in modulating the emetic response is the area postrema, the locus of the chemoreceptor trigger zone. Expand
SB‐224289–a novel selective (human) 5‐HT1B receptor antagonist with negative intrinsic activity
1 Human 5‐HT1B (h5‐HT1B) and human 5‐HT1D (h5‐HT1D) receptors show remarkably similar pharmacology with few compounds discriminating the receptors. We report here on a novel compound, SB‐224289Expand
Importance of h5-HT1B Receptor Selectivity for 5-HT Terminal Autoreceptor Activity: an In Vivo Microdialysis Study in the Freely-moving Guinea-pig
TLDR
The lack of effect of the above h5-HT1B receptor selective compounds and the decrease in extracellular 5-HT elicited by the non-selective compounds GR 127935, GR125743 and methiothepin suggest that antagonism of 5- HT1D receptors may mediate this decrease in 5-ht levels. Expand
Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species.
TLDR
There was a close correlation between drug affinities in each area of human brain, and specific binding to homogenates of rat area postrema and vagus nerve was characterised. Expand
The potential anxiolytic activity of GR38032F, a 5‐HT3‐receptor antagonist
TLDR
It is concluded that GR38032F is potentially a very potent anxiolytic agent without sedative, anticonvulsant or hypnotic activity. Expand
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