Human genetic variations in the 5HT2A receptor
Bibliographic record
Abstract
OBJECTIVE: to determine if the agonist serotonin and antagonists loxapine and clozapine have an altered potency for four allelic variants (T25N, I197V, A447V, and H452Y) of the human 5HT2A receptor when compared to the wild-type allele. METHODS: The receptor or its variants are studied in an in-vitro functional assay system consisting of a Sf9 insect cell line that is stably transformed with the human wild-type and mutant alleles. This assay system measures release of calcium stores due to receptor activation by agonists and inhibition of this agonist stimulated response by antagonists. RESULTS: Both loxapine and clozapine exhibit non-competitive antagonism of serotonin stimulation of the human 5HT2A receptor signal transduction system and loxapine is the more potent inhibitor. This study shows that the I197V allele requires a two-fold higher concentration of the atypical neuroleptic clozapine to inhibit serotonin stimulation compared to the wild-type receptor (P = 0.036). The I197V mutation does not affect the inhibition of serotonin stimulation by the typical neuroleptic loxapine nor does it alter the activation of the receptor by serotonin. It is also significant that the results of this study indicate that the T25N, A447V, and H452Y mutations in the human 5HT2A receptor do not significantly alter the response of the receptor to the agonist serotonin or the antagonists loxapine and clozapine.
Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.
How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.004 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".