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Mendeley readers
Attention Score in Context
| Title |
BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties
|
|---|---|
| Published in |
Psychopharmacology, February 1993
|
| DOI | 10.1007/bf02251279 |
| Pubmed ID | |
| Authors |
T. P. Blackburn, G. S. Baxter, G. A. Kennett, F. D. King, D. C. Piper, G. J. Sanger, D. R. Thomas, N. Upton, M. D. Wood |
| Abstract |
The novel 5-HT3 antagonist, BRL 46470A (endo-N-(8-methyl-8-azabicyclo [3.2.1]oct-3-yl)2,3-dihydro-3,3 dimethyl-indole-1-carboxamide, hydrochloride), has been investigated in a series of in vitro and in vivo tests, including the effect of the drug in models of anxiolysis. In classical tests for 5-HT3 receptor antagonism, BRL 46470A was shown to antagonise 5-HT3 mediated responses in the guinea-pig ileum [pA2 8.3 +/- 0.5, slope 0.98 +/- 0.20, mean +/- SEM (5)], the rabbit isolated heart (pA2 10.1 +/- 0.1, slope 1.2 +/- 0.2, n = 5) and the rat Bezold-Jarisch model (ID50 0.7 microgram/kg IV +/- 0.1, n = 8), with a long duration of action (> 3 h). BRL 46470A selectively displaced [3H]-BRL 43694 from 5-HT3 binding sites in rat brain membranes (Ki 0.32 nM +/- 0.04, n = 4) without displacing (at concentrations greater than 1 microM) a wide variety of ligands binding to other neurotransmitter receptors, opioid receptors and to neurotransmitter gated ion channel complexes. In vivo, BRL 46470A showed anxiolytic-like activity in two animal models predictive of antianxiety effects-elevated X-maze and social interaction in rats. In both models, BRL 46470A showed significant activity over a wide dose-range following both oral (0.0001-0.1 mg/kg PO) and systemic administration. The unique level of potency of BRL 46470A was apparent in the rat social interaction test and was shown to be 100 fold more potent than the 5-HT3 receptor antagonist ondansetron, with no evidence of a bell-shaped dose response curve over 4 orders of magnitude.(ABSTRACT TRUNCATED AT 250 WORDS) |
Mendeley readers
The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 14 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 3 | 21% |
| Student > Bachelor | 3 | 21% |
| Other | 2 | 14% |
| Librarian | 1 | 7% |
| Student > Ph. D. Student | 1 | 7% |
| Other | 1 | 7% |
| Unknown | 3 | 21% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 3 | 21% |
| Pharmacology, Toxicology and Pharmaceutical Science | 3 | 21% |
| Medicine and Dentistry | 2 | 14% |
| Social Sciences | 2 | 14% |
| Veterinary Science and Veterinary Medicine | 1 | 7% |
| Other | 0 | 0% |
| Unknown | 3 | 21% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. 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 02 April 2024.
All research outputs
#7,454,427
of 22,789,566 outputs
Outputs from Psychopharmacology
#2,099
of 5,346 outputs
Outputs of similar age
#13,102
of 65,226 outputs
Outputs of similar age from Psychopharmacology
#10
of 22 outputs
Altmetric has tracked 22,789,566 research outputs across all sources so far. This one is in the 44th percentile – i.e., 44% of other outputs scored the same or lower than it.
So far Altmetric has tracked 5,346 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 10.6. This one is in the 28th percentile – i.e., 28% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 65,226 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 20th percentile – i.e., 20% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 22 others from the same source and published within six weeks on either side of this one. This one is in the 22nd percentile – i.e., 22% of its contemporaries scored the same or lower than it.