Epibatidine and its analogues as nicotinic acetylcholine receptor agonist: an update.
Epibatidine (EPB) (1), an alkaloid isolated from the skin of the Ecuadorian poison frog, Epipedobates tricolor has attracted attention because of its exceptionally powerful analgesic properties: several hundred times greater than those of morphine, and the fact that it acts at nicotine rather than opiate receptors. Although the substance is toxic, it does serve as a lead compound in the development of drugs for pain relief as well as treatment of disorders whose pathogenesis involves nicotinic receptors. In this article, isolation, synthetic methods, effect on neuronal and neuromuscular nicotinic receptors, therapeutic potential, toxicity, nicotinic pharmacophore structural modifications related issues of 1 are discussed.
Yogeeswari
Perumal
P
Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani 333 031, India. pyogee@bits-pilani.ac.in
Sriram
Dharmarajan
D
Ratan Bal
Tanushree
T
Thirumurugan
Rathinasabapathy
R
D018712:Analgesics, Non-Narcotic / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D001001:Anura; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D018722:Nicotinic Agonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D010146:Pain / Q000188:drug therapy*; D008517:Phytotherapy; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D011978:Receptors, Nicotinic / Q000187:drug effects; D012867:Skin / Q000378:metabolism; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D019086:Bridged Bicyclo Compounds, Heterocyclic; D018722:Nicotinic Agonists; D011725:Pyridines; D011978:Receptors, Nicotinic; C082748:epibatidine