title: The efficacy of delta-opioid receptor-selective drugs.
abstract: Delta-opioid receptor-selective drugs may provide an alternative to mu-opioid-selective drugs currently used for the relief of pain. To develop improved delta-opioid receptor-selective drugs, better measures of drug activity are necessary. In this review we suggest that efficacy calculations provide a superior measure of drug activity as compared to dissociation constants and drug potencies in functional assays. Efficacy, as discussed in this review, is defined as a quantitative measurement of the ability of a drug to stimulate second messenger systems or measurable functional responses in cells or tissues under standard conditions. Efficacy values will allow medicinal chemists to understand the contributions of both the coupling efficiency and dissociation constant to drug potencies in the development of new delta-opioid receptor-selective drugs.
authors.affiliation: Department of Pharmacology, University of Arizona, Tucson 86724, USA.
authors.forename: T H
authors.initials: TH
authors.lastname: Burkey
authors.forename: F J
authors.initials: FJ
authors.lastname: Ehlert
authors.forename: Y
authors.initials: Y
authors.lastname: Hosohata
authors.forename: R M
authors.initials: RM
authors.lastname: Quock
authors.forename: S
authors.initials: S
authors.lastname: Cowell
authors.forename: K
authors.initials: K
authors.lastname: Hosohata
authors.forename: E
authors.initials: E
authors.lastname: Varga
authors.forename: D
authors.initials: D
authors.lastname: Stropova
authors.forename: X
authors.initials: X
authors.lastname: Li
authors.forename: C
authors.initials: C
authors.lastname: Slate
authors.forename: H
authors.initials: H
authors.lastname: Nagase
authors.forename: F
authors.initials: F
authors.lastname: Porreca
authors.forename: V J
authors.initials: VJ
authors.lastname: Hruby
authors.forename: W R
authors.initials: WR
authors.lastname: Roeske
authors.forename: H I
authors.initials: HI
authors.lastname: Yamamura
mesh_terms: D000700:Analgesics / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells / Q000378:metabolism; D006224:Cricetinae; D006801:Humans; D007700:Kinetics; D051379:Mice; D017465:Receptors, Opioid, delta / Q000187:drug effects* / Q000378:metabolism*
chemical_list: D000700:Analgesics; D017465:Receptors, Opioid, delta