Use of Writhing Test for Evaluating Analgesic Activity of Narcotic Antagonists

Blumberg, Harold; Wolf, Peter S.; Dayton, Hyman B.

doi:10.3181/00379727-118-29963

Cited by 78 publications

(22 citation statements)

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“…Similarly, the rank-order potency for antagonists in precipitating Sub-headings under the species refer to the Straub tail reaction in mice, abdominal constrictions produced by phenylquinone in mice, ability of the mice to stay on a rotating rod, reactions of mice on a hot plate, reactions of rats to radiant heat focused on their tails, and the relief of pain in humans. Capital letters designate the studies from which the potencies were derived: A, Present study; B, Pearl et al, 1968; see also Siegmund, Cadmus & Lu, (1957);Blumberg, Wolf & Dayton (1965); C, Eddy, Halbach & Braenden (1956); D, Archer et al (1964); Grumbach & Chemov (1965); Tullar et al (1966); E, review of literature by Lasagna (1964). Ranks in the body of the table are based on parenteral doses in mg/kg of the free base.…”

Section: Discussionmentioning

confidence: 99%

Effects of opiates and opiate antagonists on the Straub tail reaction in mice

Aceto

McKean

Pearl

1969

British J Pharmacology

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. Subcutaneous injections of opiates produced the Straub tail reaction in mice. The potencies of the opiates in mice were consistent with previous estimates of the analgesic potencies in animals and in man. . The potencies of sixteen antagonists in counteracting the reaction were consistent with those previously obtained with the rat tail‐flick test. . The (–) isomers of four benzomorphan derivatives were much more potent in counteracting the reaction than their (+) isomers and about twice as potent as their racemates. The activity of the isomers seemed to follow Pfeiffer's rule: the lower the effective dose of a drug, the greater the difference in the pharmacological effects of the optical isomers. One of the trans isomers acted like an opiate, while its cis isomer acted like an antagonist. . Naloxone and nalorphine fulfilled conventional criteria for competitive antagonism, whereas atropine and the (–) and the (+) isomers of pentazocine and of cyclazocine did not do so. . The Straub tail test seems to be useful for studying structure‐activity relations among opiates and opiate antagonists.

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Section: Discussionmentioning

confidence: 99%

Effects of opiates and opiate antagonists on the Straub tail reaction in mice

Aceto

McKean

Pearl

1969

British J Pharmacology

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“…Since the analgesic test involving the induction of writhes or stretches in rodents is quite sensitive to the effects of both the narcotics and the narcotic antagonists (Taber, Greenhouse & Irwin, 1964;Blumberg, Wolf & Dayton, 1965), it provides a convenient assay for comparative studies of these two groups of compounds. Naloxone has been reported to be a potent antagonist of both narcotic and narcoticantagonist analgesics (Blumberg, Dayton & Wolf, 1966) and to possess no analgesic activity in this assay (Blumberg, Dayton, George & Rapaport, 1961).…”

Section: Introductionmentioning

confidence: 99%

Quantitative studies on the antagonism by naloxone of some narcotic and narcotic‐antagonist analgesics

Smits

Takemori

1970

British J Pharmacology

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Summary1. Naloxone was used to study the antagonism of the analgesic effects of some narcotics (morphine sulphate, levorphanol tartrate, and methadone hydrochloride) and narcotic antagonists (pentazocine, cyclazocine, and nalorphine hydrochloride). The analgesic assay used was the mouse phenylbenzoquinone stretching test. 2. The in vivo equivalent of a pA2 value (apparent pA2) for naloxone was determined with each agonist. These values were found to be significantly larger with the narcotics than with the narcotic antagonists. 3. The slopes in the apparent pA2 plots were also found to be significantly different. It was concluded that this difference in slopes was probably not due to a lack of equilibrium in one of the two groups of analgesics. 4. The results suggest that the narcotic and the narcotic-antagonist analgesics may inhibit stretching in this assay by interacting either with two different receptors or with the same receptor in a different manner.

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“…They concluded that the response was nociceptive and they used it as a basis for testing analgesic drugs. The antinociceptive tests developed from this work have the advantage that they are sensitive to antipyretic drugs (Siegmund et al, 1957;Hendershot & Forsaith, 1959;Koster et at., 1959;Keith, 1960) and to narcotic antagonists (Taber, Greenhouse & Irwin, 1964;Blumberg, Wolf & Dayton, 1965;Pearl & Harris, 1966). These tests have, however, three disadvantages: (1) exposure of animals to peritoneal stimulation intense enough to induce repeated abdominal constrictions for longer than necessary is ethically undesirable and needlessly time consuming; (2) increased permeability of blood vessels accompanies peritoneal irritation (Northover, 1963(Northover, , 1964 and the development of abdominal constrictions (Whittle, 1963, 1964a and, and so an antinociceptive effect cannot easily be distinguished from an anti-inflammatory; and (3) the test produces many false positives (Hendershot & Forsaith, 1959;Emele & Shanaman, 1963;Brittain, Lehrer & Spencer, 1963;Okun, Liddon & Lasagna, 1963).…”

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confidence: 99%