| Title |
Etoperidone, trazodone and MCPP: in vitro and in vivo identification of serotonin 5-HT1A (antagonistic) activity
|
|---|---|
| Published in |
Psychopharmacology, August 1992
|
| DOI | 10.1007/bf02245118 |
| Pubmed ID | |
| Authors |
R. B. Raffa, R. P. Shank, J. L. Vaught |
| Abstract |
The Ki values for etoperidone, trazodone and MCPP (m-chlorophenylpiperazine dihydrochloride) at 5-HT1A sites (using rat cerebral cortical synaptosomes and [3H]8-OH-DPAT) were determined to be 20.2, 23.6 and 18.9 nM, respectively. In an effort to elucidate the functional nature of the interaction at 5-HT1A sites in vivo, the ability of each compound to elicit reciprocal forepaw treading (RFT) or to block the RFT induced by 8-OH-DPAT in reserpinized rats was tested. Specifically, 8-OH-DPAT (1.0 mg/kg SC)-challenged or non-challenged (control) reserpinized (1.0 mg/kg SC) rats were administered etoperidone, trazodone or MCPP (IP) and scored for the elicitation of RFT (indicative of 5-HT1A agonistic activity) or for block of RFT induced by 8-OH-DPAT (indicative of 5-HT1A antagonistic activity). Reference compounds confirmed the specificity of the test. We report that etoperidone, trazodone and MCPP inhibited 8-OH-DPAT-induced RFT (ID50 = 17.4, 23.8 and 13.4 mg/kg, respectively). Only marginal RFT was produced in non-challenged animals by etoperidone and trazodone at a high dose (40 mg/kg). Taken together, the results suggest a predominant antagonistic activity of etoperidone, trazodone and MCPP at 5-HT1A receptor sites in rat central nervous system. However, one cannot rule out the possibility that these compounds are weak partial agonists. This activity may be relevant to the antidepressant action of these compounds. |
Mendeley readers
The data shown below were compiled from readership statistics for 12 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 12 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Other | 2 | 17% |
| Researcher | 2 | 17% |
| Lecturer > Senior Lecturer | 1 | 8% |
| Professor | 1 | 8% |
| Student > Bachelor | 1 | 8% |
| Other | 2 | 17% |
| Unknown | 3 | 25% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 2 | 17% |
| Biochemistry, Genetics and Molecular Biology | 2 | 17% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 8% |
| Neuroscience | 1 | 8% |
| Chemistry | 1 | 8% |
| Other | 0 | 0% |
| Unknown | 5 | 42% |
Attention Score in Context
This research output has an Altmetric Attention Score of 6. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 26 September 2020.
All research outputs
#5,431,319
of 25,388,229 outputs
Outputs from Psychopharmacology
#1,346
of 5,470 outputs
Outputs of similar age
#2,290
of 18,152 outputs
Outputs of similar age from Psychopharmacology
#9
of 31 outputs
Altmetric has tracked 25,388,229 research outputs across all sources so far. Compared to these this one has done well and is in the 75th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 5,470 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 11.9. This one has gotten more attention than average, scoring higher than 68% of its peers.
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We're also able to compare this research output to 31 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 67% of its contemporaries.