Polydiscamides B-D from a marine sponge Ircinia sp. as potent human sensory neuron-specific G protein coupled receptor agonists.
Polydiscamides B, C, and D (1-3) were isolated from a sponge Ircinia sp. The structures of 1 to 3 were elucidated by the comparison of their NMR and HRESIMS spectroscopic data with that of a structurally related compound, polydiscamide A. All compounds showed potent agonist activity against human sensory neuron-specific G protein couple receptor (SNSR), a receptor involved in the modulation of pain, and they are the first examples of nonendogenous human SNSR agonists.
Feng
Yunjiang
Y
Eskitis Institute, Griffith University, Brisbane, Queensland, Australia.
Carroll
Anthony R
AR
Pass
David M
DM
Archbold
Julia K
JK
Avery
Vicky M
VM
Quinn
Ronald J
RJ
D000818:Animals; D001315:Australia; D006801:Humans; D015394:Molecular Structure; D009475:Neurons, Afferent / Q000187:drug effects*; D010147:Pain Measurement / Q000187:drug effects; D010456:Peptides, Cyclic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D011161:Porifera / Q000737:chemistry*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*
D010456:Peptides, Cyclic; D043562:Receptors, G-Protein-Coupled; C527502:polydiscamide B; C527503:polydiscamide C; C527504:polydiscamide D