Detail of "53648-55-8"

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Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids

Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids. Young, Alice M.; Stephens, Kenneth R.; Hein, David W.; Woods, James H. (Med. Sch., Univ. Michigan, Ann Arbor, MI 48202, USA). J. Pharmacol. Exp. Ther., 229(1), 118-26 (English) 1984. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Nine mixed agonist-antagonist opioids were evaluated in monkeys for their ability to serve as pos. reinforcers and their discriminative stimulus similarity to etorphine [14521-96-1] and ethylketazocine methanesulfonate [60183-11-1]. For tests of reinforcing properties, drugs were substituted for codeine under a fixed-ratio 30 time-out 600 s schedule of i.v. delivery. Discriminative properties were assessed in sep. groups of monkeys for which etorphine and saline, or ethylketazocine and saline, were established as discriminative stimuli for responses maintained under a fixed-ratio 20 schedule of food delivery. Two patterns of reinforcing and discriminative stimulus properties were obsd. Buprenorphine [52485-79-7], butorphanol tartrate [58786-99-5], GPA 1657 [21141-28-6], nalbuphine [20594-83-6], propiram fumarate [13717-04-9], and WY 16225 (dezocine) [53648-55-8] functioned as pos. reinforcers and occasioned etorphine-appropriate but not ethylketazocine-appropriate responses. dl-Profadol [1470-95-7] also functioned as a pos. reinforcer; l- [37627-70-6] and d-profadol [37627-69-3], occasioned etorphine-appropriate but not, in general, ethylketazocine-appropraite responses. In contrast, levallorphan and oxilorphan did not function as pos. reinforcers and occasioned ethylketazocine-appropriate but no more than 30% etorphine-appropriate responses. Under these exptl. conditions, the reinforcing and discriminative stimulus profiles of the mixed agonist-antagonist opioids paralleled those of etorphine-like (m) or ethylketazocine-like (k) opioid agonists.

Ventilatory and analgesic effects of dezocine in humans

Ventilatory and analgesic effects of dezocine in humans. Gal, Thomas J.; DiFazio, Cosmo A. (Med. Cent., Univ. Virginia, Charlottesville, VA 22908, USA). Anesthesiology, 61(2), 716-22 (English) 1984. CODEN: ANESAV. ISSN: 0003-3022. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The respiratory depressant and analgesic effects of i.v. dezocine [53648-55-8] were evaluated in 6 healthy volunteers. Single 0.15 mg/kg doses were compared with identical amts. of morphine [57-27-2] and the 2 drugs were given in combination. Five successive 0.15 mg/kg doses of dezocine also were given to identify dose-effect relationships. Respiratory center sensitivity was monitored by CO2 rebreathing and mouth occlusion pressure (P0.1) measurements, while analgesia to exptl. pain was tested with submaximal tourniquet ischemia. Single 0.15 mg/kg doses of dezocine produced significantly more tolerance to exptl. pain and greater respiratory depression than a comparable dose of morphine in the 1st hour, but effects of both drugs were similar thereafter. Multiple doses of dezocine progressively increased pain tolerance from 46% above control with the 1st dose to 70% above control with the 2nd dose (cumulative total 0.30 mg/kg). Addnl. dezocine doses did not result in significantly more analgesia. Depression of CO2 sensitivity followed a similar pattern. Morphine 0.15 mg/kg, when given to subjects who had received a prior dose of dezocine, produced no addnl. effect beyond that obsd. with dezocine. With the reverse sequence, dezocine increased the respiratory depression of morphine but also produced a dramatic increment in analgesia, which suggested an additive action. Dezocine is therefore an effective analgesic with morphine-like effects. In human subjects it appears to be a slightly more potent analgesic than morphine in identical clin. doses (0.15 mg/kg). Dezocine is similar to other agonist-antagonist analgesics in that it exhibits a ceiling effect for respiratory depression that parallels its analgesic activity.