Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(90)90518-V· OSTI ID:6291879

Szallasi, A; Blumberg, P M ^[1]

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1. National Institutes of Health, Bethesda, MD (USA)

Capsaicin, the pungent constituent of chili peppers, represents the paradigm for the capsaicinoids or vanilloids, a family of compounds shown to stimulate and then desensitize specific subpopulations of sensory receptors, including C-polymodal nociceptors, A-delta mechanoheat nociceptors and warm receptors of the skin, as well as enteroceptors of thin afferent fibers. An exciting recent advance in the field has been the finding that resiniferatoxin (RTX), a naturally occurring diterpene containing a homovanillic acid ester, a key structural motif of capsaicin, functions as an ultrapotent capsaicin analog. For most of the responses characteristic of capsaicin, RTX is 100-10,000 fold more potent. Structure/activity analysis indicates, however, that RTX and related homovanillyl-diterpene esters display distinct spectra of activity. Specific ({sup 3}H)RTX binding provides the first direct proof for the existence of vanilloid receptors. We expect that the RTX class of vanilloids will promote rapid progress in understanding of vanilloid structure/activity requirements and mechanism.

• OSTI ID: 6291879
• Journal Information: Life Sciences; (USA), Vol. 47:16; ISSN 0024-3205
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PROTEINS
RECEPTORS
BIOASSAY
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL PATHWAYS
NERVE CELLS
PEPPERS
STRUCTURE-ACTIVITY RELATIONSHIPS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMAL CELLS
FOOD
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
PLANTS
REACTION KINETICS
SOMATIC CELLS
VEGETABLES
550201* - Biochemistry- Tracer Techniques