Trial reportJournal of clinical pharmacology2012
Pharmacokinetics and pharmacodynamics of MK-5046, a bombesin receptor subtype-3 (BRS-3) agonist, in healthy patients.
Trial report in Journal of clinical pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
23 citing papers in PubMed.
- Identification of a Novel Antagonist of BRS-3 from Natural Products and Its Protective Effects Against HInternational journal of molecular sciences · 2025Article
- Article
- Bombesin Receptor Subtype-3 Regulates Tumor Growth by HER2 Tyrosine Phosphorylation in a Reactive Oxygen Species-Dependent Manner in Lung Cancer Cells.Targets (Basel) · 2025Article
- Neuropeptidergic systems in psychiatric disorders.Frontiers in endocrinology · 2025Review
- Orphan G protein-coupled receptors: the ongoing search for a home.Frontiers in pharmacology · 2024Review
- The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3.The Journal of pharmacology and experimental therapeutics · 2022Article
- Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy.Frontiers in endocrinology · 2021Review
- Brs3 neurons in the mouse dorsomedial hypothalamus regulate body temperature, energy expenditure, and heart rate, but not food intake.Nature neuroscience · 2018Article
- Receptor-specific crosstalk between prostanoid E receptor 3 and bombesin receptor subtype 3.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2018Article
- A possible new target in lung-cancer cells: The orphan receptor, bombesin receptor subtype-3.Peptides · 2018Article
- Bombesin-like receptor 3 (Brs3) expression in glutamatergic, but not GABAergic, neurons is required for regulation of energy metabolism.Molecular metabolism · 2017Article
- Molecular basis for high affinity and selectivity of peptide antagonist, Bantag-1, for the orphan BB3 receptor.Biochemical pharmacology · 2016Article
- Bombesin-Like Receptor 3: Physiology of a Functional Orphan.Trends in endocrinology and metabolism: TEM · 2016Review
- Altered gut and adipose tissue hormones in overweight and obese individuals: cause or consequence?International journal of obesity (2005) · 2016Review
- Bombesin-like receptor 3 regulates blood pressure and heart rate via a central sympathetic mechanism.American journal of physiology. Heart and circulatory physiology · 2016Article
- Article
- Review
- Effect of bombesin receptor subtype-3 and its synthetic agonist on signaling, glucose transport and metabolism in myocytes from patients with obesity and type 2 diabetes.International journal of molecular medicine · 2015Article
- Bombesin receptor subtype 3 as a potential target for obesity and diabetes.Expert opinion on therapeutic targets · 2015Review
- Regulation of body temperature and brown adipose tissue thermogenesis by bombesin receptor subtype-3.American journal of physiology. Endocrinology and metabolism · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
Abstract
MK-5046 is an orally active, potent, selective agonist of the orphan G protein-coupled receptor bombesin receptor subtype-3 (BRS-3) that is under evaluation for treatment of obesity. We report the safety, tolerability, pharmacokinetics, and pharmacodynamics of oral doses of MK-5046 (10-160 mg) in a double-blind, randomized, placebo-controlled study in healthy and obese male volunteers. MK-5046 exposure increased dose proportionally, and MK-5046 was eliminated with an apparent terminal half-life of 1.5 to 3.5 hours. Single doses transiently increased blood pressure. Patients reported adverse events (erections and feeling hot, cold, and/or jittery) that coincided with time of occurrence (T(max)) and increased with increasing dose. No changes were observed in body temperature, heart rate, plasma glucose levels, or feelings of hunger/satiety. The blood pressure and thermal experiences attenuated with a second dose 6 hours after the first. Additionally, the erections suggest a possible, unanticipated, role for BRS-3 in reproductive physiology. Oral administration of MK-5046 achieves plasma concentrations that are projected to activate BRS-3 and therefore should be suitable for exploring its biological role in humans.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.