Short communicationCapsazepine as a selective antagonist of capsaicin-induced activation of C-fibres in guinea-pig bronchi
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Cited by (42)
Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain
2023, European Journal of Medicinal ChemistryCitation Excerpt :Moreover, it is accumulated in dorsal root ganglion neurons and adult rat vagus nerves. It is a valuable pharmacological tool for studying the capsaicin action mechanisms and capsaicin-sensitive neurons functions [110]. The structure-activity relationship of a series of capsazepine analogs synthesized by restricting the capsazepine conformation was investigated due to the lack of information on the vanillic acid-binding pocket on TRPV1 at the time [111].
Tiotropium modulates transient receptor potential V1 (TRPV1) in airway sensory nerves: A beneficial off-target effect?
2014, Journal of Allergy and Clinical ImmunologyCitation Excerpt :Further evidence for this “nontypical” interaction is the apparent lack of effect of tiotropium on capsaicin-induced contraction of isolated guinea pig trachea and bronchospasm induced in the in vivo single-fiber recording model in which tiotropium reduced capsaicin-induced afferent fiber firing without modulating the changes in bronchospasm. The contraction/bronchospasm observed in these 2 systems is thought to be through capsaicin acting on TRPV1 channels on nerves and causing the local release of substance P, which then acts on neurokinin receptors on the airway smooth muscle causing it to contract.35,36 A classical TRPV1 antagonist would be expected to modulate these responses; indeed, here we have shown that JNJ-17203212 inhibits capsaicin-induced contraction in guinea pig airways.
Novel drug targets for asthma and COPD: Lessons learned from invitro and invivo models
2014, Pulmonary Pharmacology and TherapeuticsCitation Excerpt :Studies exploring the role of TRPV1 in AHR and allergic inflammation have produced conflicting results. Contraction of isolated guinea pig ASM by TRPV1 agonists was demonstrated to involve the release of sensory neuropeptides from finite stores in nerve endings which consequently act upon neurokinin receptors on ASM, resulting in contraction [129]. Rehman et al. (2013) reported that TRPV1 modulation inhibits inflammation, AHR and airway remodeling in their IL-13 driven murine model [130].
Role of TRPV1 receptors on panic-like behaviors mediated by the dorsolateral periaqueductal gray in rats
2013, Pharmacology Biochemistry and BehaviorCitation Excerpt :Accordingly, previous work from our group showed that intra-dlPAG administration of TRPV1 antagonists also caused a panicolytic-like effect in escape reactions induced by electrical stimulation of dlPAG (Casarotto et al., 2012). Capsazepine acts as a competitive antagonist in a variety of bioassays, blocking the effects of capsaicin, a potent agonist of these receptors (Belvisi et al., 1992; Dickenson and Dray, 1991; Seno and Dray, 1993). Nonetheless, we cannot exclude the involvement of other targets in capsazepine effects, since it may also block different channels of the TRP family, including TRPM8 (Malkia et al., 2009; Xing et al., 2007).
Modulation of sensory nerve function and the cough reflex: Understanding disease pathogenesis
2009, Pharmacology and TherapeuticsDiscovery of a potent and long-acting bronchorelaxing capsazepinoid, RESPIR 4-95
2008, Pulmonary Pharmacology and Therapeutics