ArticleBritish journal of pharmacology2012
Structure-activity relationships of vanilloid receptor agonists for arteriolar TRPV1.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 53 citations in OpenAlex.
- Is the Quantity of Capsaicin in Food Related to Its Organoleptic and Sensory Effects? A Systematic Review.Food science & nutrition · 2026Review
- Functional crosstalk between the vanilloid and endocannabinoid systems in modulating vascular tone: implications for (neuro)vascular disorder therapy.The journal of headache and pain · 2025Article
- Role of transient receptor potential channels in the regulation of vascular tone.Drug discovery today · 2024Review
- Functional Analysis of TRPA1, TRPM3, and TRPV1 Channels in Human Dermal Arteries and Their Role in Vascular Modulation.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Progesterone distribution in the trigeminal system and its role to modulate sensory neurotransmission: influence of sex.The journal of headache and pain · 2023Article
- The Vanilloid (Capsaicin) Receptor TRPV1 in Blood Pressure Regulation: A Novel Therapeutic Target in Hypertension?International journal of molecular sciences · 2023Review
- Article
- Identification of a Partial and Selective TRPV1 Agonist CPIPC for Alleviation of Inflammatory Pain.Molecules (Basel, Switzerland) · 2022Article
- TRPV1 in arteries enables a rapid myogenic tone.The Journal of physiology · 2022Article
- Insulin sensitizes neural and vascular TRPV1 receptors in the trigeminovascular system.The journal of headache and pain · 2022Article
- Review
- Endothelin-1 potentiates TRPV1-mediated vasoconstriction of human adipose arterioles in a protein kinase C-dependent manner.British journal of pharmacology · 2021Article
- Vascular Dysfunction in Diabetes and Obesity: Focus on TRP Channels.Frontiers in physiology · 2021Review
- TRPV1 expressed throughout the arterial circulation regulates vasoconstriction and blood pressure.The Journal of physiology · 2020Article
- Article
- Beyond Neuronal Heat Sensing: Diversity of TRPV1 Heat-Capsaicin Receptor-Channel Functions.Frontiers in cellular neuroscience · 2020Review
- The Role of Transient Receptor Potential Vanilloid 1 in Common Diseases of the Digestive Tract and the Cardiovascular and Respiratory System.Frontiers in physiology · 2019Review
- Glycogen phosphorylase inhibition improves beta cell function.British journal of pharmacology · 2018Article
- TRPVExperimental physiology · 2017Article
- Sex-dependent expression of TRPV1 in bladder arterioles.American journal of physiology. Renal physiology · 2016Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe transient receptor potential vanilloid 1 (TRPV1) plays a role in the activation of sensory neurons by various painful stimuli and is a therapeutic target. However, functional TRPV1 that affect microvascular diameter are also expressed in peripheral arteries and we attempted to characterize this receptor. EXPERIMENTAL APPROACH: Sensory TRPV1 activation was measured in rats by use of an eye wiping assay. Arteriolar TRPV1-mediated smooth muscle specific responses (arteriolar diameter, changes in intracellular Ca(2+)) were determined in isolated, pressurized skeletal muscle arterioles obtained from the rat and wild-type or TRPV1(-/-) mice and in canine isolated smooth muscle cells. The vascular pharmacology of the TRPV1 agonists (potency, efficacy, kinetics of action and receptor desensitization) was determined in rat isolated skeletal muscle arteries. KEY
resultsCapsaicin evoked a constrictor response in isolated arteries similar to that mediated by noradrenaline, this was absent in arteries from TRPV1 knockout mice and competitively inhibited by TRPV1 antagonist AMG9810. Capsaicin increased intracellular Ca(2+) in the arteriolar wall and in isolated smooth muscle cells. The TRPV1 agonists evoked similar vascular constrictions (MSK-195 and JYL-79) or were without effect (resiniferatoxin and JYL-273), although all increased the number of responses (sensory activation) in the eye wiping assay. Maximal doses of all agonists induced complete desensitization (tachyphylaxis) of arteriolar TRPV1 (with the exception of capsaicin). Responses to the partial agonist JYL-1511 suggested 10% TRPV1 activation is sufficient to evoke vascular tachyphylaxis without sensory activation. CONCLUSIONS AND IMPLICATIONS: Arteriolar TRPV1 have different pharmacological properties from those located on sensory neurons in the rat.
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