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TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate.
Neuropharmacology. 2003 Jun; 44(7):958-67.N

Abstract

Capsiate is a capsaicin-like ingredient of a non-pungent cultivar of red pepper, CH-19 sweet. To elucidate the mechanisms underlying the non-pungency of capsiate, we investigated whether capsiate activates the cloned capsaicin receptor, TRPV1 (VR1). In patch-clamp experiments, capsiate was found to activate TRPV1 expressed transiently in HEK293 cells with a similar potency as capsaicin. Capsiate induced nociceptive responses in mice when injected subcutaneously into their hindpaws with a similar dose dependency as capsaicin. These data indicate that the non-pungent capsiate is an agonist for TRPV1 and could excite peripheral nociceptors. In contrast to this, capsiate did not induce any significant responses when applied to the skin surface, eye or oral cavity of mice, suggesting that capsiate requires direct access to nerve endings to exhibit its effects. Capsiate was proved to have high lipophilicity and to be easily broken down in normal aqueous conditions, leading to less accessibility to nociceptors. Another highly lipophilic capsaicin analogue, olvanil, was similar to capsiate in that it did not produce irritant responses when applied to the skin surface, although it could activate TRPV1. Taken together, high lipophilicity and instability might be critical determinants for pungency and so help in understanding the effects of capsaicin-related compounds.

Authors+Show Affiliations

Department of Physiology, Mie University School of Medicine, Tsu, Mie 514-8507, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

12726827

Citation

Iida, T, et al. "TRPV1 Activation and Induction of Nociceptive Response By a Non-pungent Capsaicin-like Compound, Capsiate." Neuropharmacology, vol. 44, no. 7, 2003, pp. 958-67.
Iida T, Moriyama T, Kobata K, et al. TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate. Neuropharmacology. 2003;44(7):958-67.
Iida, T., Moriyama, T., Kobata, K., Morita, A., Murayama, N., Hashizume, S., Fushiki, T., Yazawa, S., Watanabe, T., & Tominaga, M. (2003). TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate. Neuropharmacology, 44(7), 958-67.
Iida T, et al. TRPV1 Activation and Induction of Nociceptive Response By a Non-pungent Capsaicin-like Compound, Capsiate. Neuropharmacology. 2003;44(7):958-67. PubMed PMID: 12726827.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate. AU - Iida,T, AU - Moriyama,T, AU - Kobata,K, AU - Morita,A, AU - Murayama,N, AU - Hashizume,S, AU - Fushiki,T, AU - Yazawa,S, AU - Watanabe,T, AU - Tominaga,M, PY - 2003/5/3/pubmed PY - 2003/8/5/medline PY - 2003/5/3/entrez SP - 958 EP - 67 JF - Neuropharmacology JO - Neuropharmacology VL - 44 IS - 7 N2 - Capsiate is a capsaicin-like ingredient of a non-pungent cultivar of red pepper, CH-19 sweet. To elucidate the mechanisms underlying the non-pungency of capsiate, we investigated whether capsiate activates the cloned capsaicin receptor, TRPV1 (VR1). In patch-clamp experiments, capsiate was found to activate TRPV1 expressed transiently in HEK293 cells with a similar potency as capsaicin. Capsiate induced nociceptive responses in mice when injected subcutaneously into their hindpaws with a similar dose dependency as capsaicin. These data indicate that the non-pungent capsiate is an agonist for TRPV1 and could excite peripheral nociceptors. In contrast to this, capsiate did not induce any significant responses when applied to the skin surface, eye or oral cavity of mice, suggesting that capsiate requires direct access to nerve endings to exhibit its effects. Capsiate was proved to have high lipophilicity and to be easily broken down in normal aqueous conditions, leading to less accessibility to nociceptors. Another highly lipophilic capsaicin analogue, olvanil, was similar to capsiate in that it did not produce irritant responses when applied to the skin surface, although it could activate TRPV1. Taken together, high lipophilicity and instability might be critical determinants for pungency and so help in understanding the effects of capsaicin-related compounds. SN - 0028-3908 UR - https://www.unboundmedicine.com/medline/citation/12726827/TRPV1_activation_and_induction_of_nociceptive_response_by_a_non_pungent_capsaicin_like_compound_capsiate_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S002839080300100X DB - PRIME DP - Unbound Medicine ER -