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PubMed1967

Conditioned suppression by a stimulus associated with nalorphine in morphine-dependent monkeys.

Three rhesus monkeys, physically dependent on morphine, were trained to press a lever for food on a fixed ratio of 10 responses. A tone, initially a neutral stimulus, was aperiodically presented every third or fourth session, 5 min before and after the intravenous injection of nalorphine, a morphine antagonist which produces an immediate withdrawal syndrome in morphine-dependent monkeys. After several sessions, conditioned suppression of food-lever response rate was observed. Conditioned bradycardia, emesis, and excessive salivation also occurred. In 40 to 45 sessions the conditioned suppression of food-lever response rate and the conditioned autonomic changes were extinguished by presenting pairings of a tone and saline injection. The monkeys were then reconditioned by presenting the tone aperiodically, every third or fourth session, 5 min before and after the intravenous injection of nalorphine. Results were similar to the initial conditioning sessions. Two rhesus monkeys not dependent on morphine were stabilized on a food schedule similar to that used for the first three monkeys. These monkeys showed no change in food-lever response rate during or after nalorphine injections.

Animals↗

PubMed1990

Butorphanol, levallorphan, nalbuphine and nalorphine as antagonists in the squirrel monkey.

The effects of several mixed-action opioid agonist/antagonists were examined alone and in combination with the mu-opioid agonist l-methadone and the kappa-opioid agonist, trans-3,4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)cyclohexyl]benzeneace tam ide (U50,488). Effects were examined in squirrel monkeys responding under a schedule of shock titration. Under this procedure shock was scheduled to increase once every 15 sec from 0.01 to 3.7 mA in 30 steps. Five responses on a lever during the 15-sec shock period terminated the shock for 15 sec, after which the shock resumed at the next lower intensity. The intensity below which the monkeys maintained the shock 50% of the time (median shock level) was determined. l-Methadone and U50,488 produced dose-dependent increases in median shock level. Nalbuphine, butorphanol and levallorphan also increased median shock level, but these increases were much smaller than those observed with l-methadone or U50,488. Nalorphine and naltrexone did not increase median shock level. Butorphanol, levallorphan, nalbupine, nalorphine and naltrexone all produced parallel, rightward shifts in both the l-methadone and U50,488 dose-effect curves. The apparent pA2 values obtained for naltrexone in combination with l-methadone (7.7) were at least one log unit larger than those obtained for naltrexone in combination with U50,488 (6.5). Similar differences were revealed for nalbuphine in combination with l-methadone (6.1) and U50,488 (5.2) as well as for nalorphine in combination with l-methadone (6.0) and U50,488 (5.5).(ABSTRACT TRUNCATED AT 250 WORDS)

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗

PubMed1968

Detection of narcotic use. Comparison of the nalorphine (pupil) test with chemical tests.

The nalorphine (pupil) test for narcotic abuse is widely used in California. It is based on the ability of nalorphine to produce mydriasis in subjects who have recently taken morphine-like drugs and to produce miosis in others. The test will usually detect as little as 15 mg of morphine or comparable doses of other narcotics for several hours except in special circumstances. It is even more reliable for detection of chronic use of narcotics. A simple card pupillometer is adequate for measuring changes in pupil size resulting from nalorphine. Analysis for narcotics in urine by thin layer chromatography is also used, either alone or in conjunction with the pupil test, to detect drug abuse. In one study which included many urine speciments from subjects who had negative pupil tests the correlation between the pupil test and urinalysis was good (85 percent). When urinalysis was used to confirm suspicion of drug use resulting from a positive or equivocal pupil test, inter-method agreement dropped to about 50 percent for various reasons. Even so, use of the pupil test for screening and urinalysis for confirmation provides a satisfactory program for detection of narcotic abuse.

Chromatography, Thin Layer↗

PubMed1982

Temporal variations in the effect of morphine and nalorphine on total brain acetylcholine content in the rat.

The effect of increasing doses of morphine and nalorphine on total rat brain acetylcholine (ACh) content was determined 30 min after the administration of the drugs at 07h30 and 19h30. The results indicate that the effects of morphine and nalorphine on brain ACh levels varied depending upon the time of administration. For instance, 10 mg/kg of morphine did not significantly change total brain ACh when injected in the morning whereas a 45% increase in ACh level was observed after administration of the same dose at night. Depending on the time of administration, nalorphine increased or decreased ACh content of rat brain. The results are discussed and related to the circadian rhythms that were demonstrated in brain levels of ACh, in opioid receptors and in the secretion of opioid peptides.

Acetylcholine↗

PubMedDate not supplied

[Comparative evaluation of the protective action of nalorphine and pentazocine in acute morphine and promedol poisoning].

It was shown in experiments on white rats that the intensity of the antitoxic action of nalorphine (0.57 mg/kg) and pentazocin (3 mg/kg) is related to the chemical structure of a narcotic analgetic agent. This action is more clearly manifested during poisoning induced by the phenylpiperidine derivative promedol (LD50 33.33 mg/kg). Nalorphine increases LD50 of promedol and corrects of metabolic disturbances produced by promedol. Pentazocin does not compare favourably to nalorphine since it mostly acts as a stimulant of external respiration.

Acid-Base Equilibrium↗

PubMed1976

The effects of morphine and nalorphine-like drugs in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog.

A series of morphine-like and nalorphine-like drugs were studied in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog. In the nondependent dog, three profiles of activity were found which could be utilized to distinguish between morphine, WIN 35, 197-2 and cyclazocine. Propiram, a prototypic partial agonist of the morphine type, produced morphine-like effects in nondependent dogs and both precipitated and suppressed abstinence in cyclazocine-dependent dogs as was needed to precipitate abstinence in morphine-dependent dogs. WIN 35, 197-2, a strong agonist in the guinea-pig ileum which has been shown to be resistant to antagonism by naloxone, neither precipitated nor suppressed morphine abstinence but suppressed cyclazocine abstinence. In the nondependent dog, it depressed the flexor reflex but not skin twitch reflex. Cyclazocine altered reflex activity much like WIN 35, 197-2 but produced tachycardia, tachypnea, mydriasis and canine delirum. The morphine and cyclazocine precipitated and withdrawal abstinence syndromes were qualitatively different. Twenty times as much naltrexone was needed to precipitate abstinence in morphine-dependent dogs. Nalorphine both precipitated and suppressed cyclazocine abstinence and appeared to be a partial agonist of the nalorphine-type. Morphine suppressed the cyclazocine abstinence syndrome. Cross-tolerance was not observed in ketocyclazocine-dependent dogs. These data are consistent with the hypothesis that there are strong and partial agonists of the mu and kappa types, and further, that physical dependence on morphine and cyclazocine is mediated through different receptors. WIN 35, 197-2 appears to be a pure strong agonist of the kappa type. Cyclazocine is a mu antagonist and mixed kappa and sigma agonist.

Animals↗

PubMed1981

Effects of morphine and nalorphine on kainic acid-induced hypothermia in rats.

Intraventricular administration of kainic acid at the dose of 0.1 microgram induces a significant depression of rectal temperature followed rapidly by its slight elevation. Morphine (40.0 mg.kg-1 IP), which by itself elicited biphasic effect on the body temperature of rats--initially hypothermia followed by hyperthermia--slightly increased the kainic acid-induced hypothermia. Kainic acid did not cause any changes in the hyperthermic effect of low doses of morphine (10.0 mg.kg-1). Pretreatment of rats with nalorphine enhanced the kainic acid-induced hypothermia. On the contrary, nalorphine reversed the hypothermic effect produced by morphine at the dose of 40.0 mg.kg-1. The results suggest that morphine and kainic acid-induced hypothermia are not mediated by the influence on the same type of receptors.

Animals↗

PubMed1985

Behavioral effects of naloxone and nalorphine preceding and following morphine maintenance in the rhesus monkey.

The effects of morphine, naloxone, and nalorphine on responding maintained under a variable-interval schedule of food presentation were assessed in rhesus monkeys before and after successive periods of daily morphine maintenance (15.0 mg/kg/day SC). Withdrawal from morphine dependence was accomplished gradually following the first two maintenance periods and abruptly following the third period. Schedule-controlled responding was disrupted when morphine maintenance was abruptly discontinued but not when the maintenance dosage was gradually reduced to zero. Tolerance to the acute effects of IV morphine on responding developed during morphine maintenance and dissipated after daily injections were discontinued. The effects of IV naloxone and IV nalorphine following each period of morphine maintenance were generally similar to their effects in initial determinations. These data indicate that tolerance-producing regimens of repeated daily injections with morphine do not necessarily produce enduring changes in the effects of opiate antagonists on schedule-controlled behavior. Additionally, gradual withdrawal from morphine maintenance can minimize the behavioral disruptions that attend abrupt abstinence.

Animals↗

PubMed1980

Nalorphine's effect under several schedules of electric shock titration.

The effects of nalorphine were examined under a shock titration procedure in which squirrel monkeys received shock during 15-s period. If the monkey did not make five responses during the 15-s shock period, the shock was increased by one increment and maintained for another 15-s period. If five responses were made during the 15-s shock period, the shock was immediately terminated for 15s during which the chamber was dark (time out). After the 15-s time out period, the shock resumed at the next lower intensity. Three schedules of shock increment were examined in which shock increased from 0 to either 1.0, 2.0, or 5.5 mA. Under all three schedules of shock increment nalorphine decreased median shock levels and increased rates of responding in the presence of shock and in the absence of shock (i.e., during time out). These effects were apparent during hour 1 of the session. Responding during hours 2 and 3 of the session was unchanged.

Animals↗

PubMed1977

The effect of the narcotic antagonists naloxone, naltrexone and nalorphine on spinal cord C-fiber reflexes evoked by electrical stimulation or radiant heat.

C-fiber reflexes were recorded from an S1 ventral root in the acute decerebrate low spinal cat following stimulation of the ipsilateral superficial peroneal nerve or application of radiant heat to the metacarpel footpad. Naloxone when administered i.v. increased the electrically evoked C-fiber reflex to 158% (+/- 23.8% S.E.M.) of control 10 min after administration; whereas, naltrexone, 0.0025 mg/kg, increased the C-fiber reflex to 206 +/- 26.1% (S.E.M.) of control. Naloxone in a dose of 0.050 mg/kg increased the radiant heat evoked ventral root reflext to 161 +/- 19.5% of control. Nalorphine, 1 mg/kg, facilitated the electrically evoked C-fiber reflex to 282 +/- 75% of control. These findings that naloxone and naltrexone facilitated these reflexes in doses too small to have non-specific excitatory effects and that nalorphine facilitated the C-fiber reflex at a dose level that is depressant to the flexor reflex in the chronic spinal dog are consistent with a hypothesis that these effects are due to antagonism of a naturally occurring opiate-like inhibitory substance.

Action Potentials↗

PubMed1976

A comparison in mice of naloxone and nalorphine as antagonists to neuroleptanalgesic drugs.

The effectiveness of naloxone and nalorphine in antagonizing the effects of fentanyl and droperidol on the hot plate reaction time and the respiratory rate of the mouse has been compared. Naloxone was superior to nalorphine, being a more effective antagonist, and was also free from significant agonist effects. However, neither antagonist was completely effective against the respiratory rate depression produced by combinations of fentanyl and droperidol. It is suggested that the duration of the antagonist effects of naloxone are shorter against respiratory depression than against analgesia.

Animals↗

PubMed1971

Cardiovascular effects of morphine, pethidine, diamorphine and nalorphine on the cat and rabbit.

1. The predominant effect of morphine, diamorphine, pethidine or nalorphine on the blood pressure of the anaesthetized cat or rabbit is hypotension although, occasionally, a pressor action may predominate or intervene.2. Possible mechanisms of the depressor phases of action have been studied on cardiac and vascular preparations both in situ and in vitro.3. While in the whole animal, catecholamine release from the adrenal medulla and histamine liberation may be implicated in the responses, the vasodilator and vascular relaxant actions of morphine and, probably, pethidine, nalorphine and diamorphine on the isolated preparations are not mediated by the liberation of known peripheral transmitters or autacoids or by interaction with their specific receptors.

Acetylcholine↗

PubMed1972

Effects of pethidine and nalorphine on the mechanical and electrical activities of mammalian isolated ventricular muscle.

1. The strength of the isometric mechanical contraction of electricallydriven ventricular muscle has been recorded simultaneously with the resting and action potentials; the effects of pethidine and of nalorphine on these parameters have been studied.2. When lower concentrations of pethidine (0.22-6.5 mug/ml) were perfused, isometric peak tension was decreased in parallel with the maximum upstroke velocity of the action potential; these actions are considered to result from membrane stabilization. At higher concentrations (11.8-109 mug/ml) pethidine usually produced, in addition, a progressive decrease in the resting and action potentials associated with marked irregularities in, or even abolition of, the mechanical response. It is suggested that these effects of the higher doses might be due to a depression of ATPase activity in the myocardial membrane.3. Compared with pethidine, nalorphine had similar, but weaker, actions.

Action Potentials↗

PubMed1989

Effects of propranolol, nalorphine and haloperidol on the breathing and on the metabolism of PGI2 and TXA2 of normotensive and spontaneously hypertensive rats.

The influence of propranolol, nalorphine and haloperidol on the breathing pattern and on the blood levels of cyclooxygenase products of anaesthetized spontaneously-breathing normotensive Wistar rats (WR) and of spontaneously hypertensive rats (SHR) were investigated. The respiratory rate was higher and the effective lung resistance was smaller in the SHR than in the WR. Breathing frequency decreased after nalorphine in both groups, while only in SHR after haloperidol. Propranolol augmented the dynamic lung resistance in both groups. The blood 6-keto-PGF1 alpha level was higher and the TXB2 level was lower in the SHR than in the WR. The central inspiratory activity as well as the levels of peripherally acting substances involved in the regulation of respiration and in the control of bronchial smooth muscle tone are different in the SHR and WR.

Animals↗

PubMed1988

Peripheral modulation of pain in conscious guinea pigs: effect of morphine, nalorphine and clonidine.

1. Morphine and nalorphine were shown to have a peripheral analgesic effect on conscious guinea pigs, producing a decrease in the vocalization response to noxious electrical stimulation. Naloxone antagonized the effect of morphine and nalorphine. 2. Locally administered clonidine had a peripheral analgesic effect on conscious guinea pigs, producing a decrease in the vocalization response to noxious electrical stimulation. 3. The peripheral analgesia of clonidine was antagonized by yohimbine and naloxone. The analgesic effect of clonidine was 250-300 times more potent than that of lidocaine. 4. It is suggested that alpha 2-adrenergic receptor agonists may activate enkephalin-like substances released at the peripheral level.

Analgesia↗

PubMed1987

[Functioning of the pituitary-adrenal system during the vestibulo-vegetative syndrome and administration of dalargin and nalorphine].

Changes in ACTH, cortisol, beta-endorphin have been investigated during vestibulo-vegetative syndrome (VVS) and injections of dalargin (leu-enkephalin analog) and nalorphine (agonist-antagonist of opioid receptors) in 9 volunteers with low level vestibulo-vegetative stability. Cumulative coriolis acceleration test during rotations on a special chair was used for VVS modelling. Dalargin (1-4 mg), nalorphine (5 mg) and placebo (NaCl solution) were injected intravenously 5-15 min before rotation. A significant increase in ACTH, cortisol and beta-endorphin plasma levels has been observed. Mean positive linear correlation (r greater than +0.6) between ACTH and beta-endorphin and ACTH and cortisol was noted immediately after the test only when dalargin was injected. It is suggested that in VVS there develops a hormonal conflict, i. e. an adequate hormonal release is disturbed.

Autonomic Nervous System Diseases↗

PubMed1981

Effects of morphine, nalorphine and morphine withdrawal on lethal toxicity of intracerebroventricular kainic acid in mice.

The effects of morphine, nalorphine and morphine withdrawal on intracerebroventricular kainic acid (0.1 and 0.2 micrometers) lethal toxicity were examined. Morphine (40 mg/kg) potentiated the lethal effect of a low (0.1 micrometer) but not that of a higher dose (0.2 micrometer) of kainic acid. Nalorphine (20 mg/kg) did not affect the toxic action of kainic acid. The mice during morphine withdrawal were very sensitive to the lethal effects of both doses of the amino acid. Kainic acid toxicity seems to be closely related to the functional state of the opiate system. Moreover, it seems that in tolerant animals a supersensitivity of glutamatergic receptors is likely to occur.

Animals↗

PubMed1981

The antagonistic effect of pentazocine on fentanyl induced respiratory depression compared with nalorphine and naloxone.

The effect of pentazocine, a strong analgesic with a weak opiate antagonistic activity, on fentanyl-induced respiratory depression was studied after anaesthesia in patients undergoing gynaecological laparotomy. Pentazocine (1 mg/kg) was given intravenously at the end of operation. The postoperative respiratory depression in these patients was compared with that in patients who received strong opiate antagonists, nalorphine and naloxone, or no opiate antagonists. Respiratory depression was evaluated by measuring respiratory rate, respiratory minute volume and blood gases. The results show that pentazocine has a clear antagonistic effect on fentanyl-induced respiratory depression but the effect of 1 mg/kg is weaker and shorter than that produced by 5 mg of nalorphine or 0.4 mg of naloxone. Postoperative analgesia in patients who received pentazocine was not longer than that in patients who received no opiate antagonists at the end of the operation.

Adult↗