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Biomedical subjects

C Castellano

Publications and source records attributed to C Castellano.

At least 91 records · Page 5Linked to original sources

Tripelennamine enhances buprenorphine-, but not pentazocine-induced hyperactivity in mice.

The opioid agonist-antagonist pentazocine (1-30 mg/kg) and the partial agonist buprenorphine (0.05-0.25 mg/kg) were tested, alone or in combination with the histamine H1-receptor antagonist tripelennamine (1, 2.5, 5 or 10 mg/kg), on locomotor activity in mice of the CD-1 strain. When given alone, pentazocine produced slight and non-dose-related activity increments, while buprenorphine induced strong and dose-related locomotor stimulation. Tripelennamine slightly increased activity by itself and enhanced buprenorphine-, but not pentazocine-induced hyperactivity. The results are discussed in relation to the hypothesis that antihistaminic agents specifically interfere with locomotor effects of opioids.

Animals↗

Chronic cocaine enhances defensive behaviour in the laboratory mouse: involvement of D2 dopamine receptors.

C57BL/6 male mice injected with a challenge dose (20 mg/kg) of cocaine 72 h after the end of chronic intermittent treatment with the psychostimulant (two daily injections of 20 mg/kg for 10 days) exhibited a clear-cut increase in defensive upright and sideways postures and escape when confronted with a non-drugged conspecific. Treated mice spent 40% of time showing defensive acts over the 5-min testing session. Administration of the selective D2 receptor antagonist (-)-sulpiride (25 mg/kg) before the challenge dose of cocaine completely antagonized the increase in defensive behaviour, while the selective D1 receptor antagonist SCH 23390 (0.25-0.50 mg/kg) did not significantly affect defensive behavioural patterns. These results suggest the involvement of D2 receptors in cocaine-induced hyperdefensiveness. The hypothesis that alteration in D2 receptor functioning produced by chronic cocaine administration may produce hyperdefensiveness possibly due to altered perceptive processes is discussed.

Animals↗

Effects of ethanol on passive avoidance behavior in the mouse: involvement of GABAergic mechanisms.

A passive avoidance methodology was used to test the effect of ethanol, and its interference with GABAergic mechanisms, on memory in male CD1 mice. Retention performance was reduced in a dose-related manner, by ethanol and by muscimol, a GABA agonist, while it was increased by the GABA antagonists picrotoxin and bicuculline. These effects were evident when treatments were carried out immediately, but not 120 min, after training, suggesting that they were due to a specific action of the drugs on the time-dependent memory consolidation process. The ethanol-induced reduction of retention performance was enhanced by muscimol and decreased by picrotoxin and bicuculline administrations. Taken together the results confirm the involvement of a GABAergic mechanism in memory consolidation and demonstrate that it underlies the negative effect of ethanol on passive avoidance behavior in the mouse.

Animals↗

The amygdala mediates the impairing effect of the selective kappa-opioid receptor agonist U-50,488 on memory in CD1 mice.

The effect of the selective kappa-opioid receptor agonist U-50,488 on passive avoidance behaviour was studied in CD1 mice bearing lesions of the amygdaloid complex. The results have shown that post-trial injections of U-50,488 in unoperated mice as well as lesions of the amygdaloid complex in untreated mice decreased retention performances. No further impairment was observed in lesioned mice treated with U-50,488, indicating that amygdala is involved in the mediation of the effects of kappa-opioid receptor agonists on memory. The possibility that kappa-opioid receptors could modulate the memory retention of CD1 mice by influencing their emotional state is discussed.

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

New analogs of physostigmine: alternative drugs for Alzheimer's disease?

The synthesis of a series of physostigmine analogs, in which the methylcarbamyl group has been substituted with monoalkylcarbamyl, dimethyl- and diethylcarbamyl groups, is reported. These compounds were prepared with the aim of investigating their possible therapeutic effects in the treatment of Alzheimer's type dementia. The new analogs of physostigmine are inhibitors of acetylcholinesterase from Electroforus electricus, with a value of the reactivation constant, k3 smaller than the one of physostigmine. The percentage of anticholinesterase activity in vitro and in vivo, the acute toxicity and some behavioural effects were also evaluated for selected derivatives. The reactivation constant, in vitro, supports the view that the derivatives described would be more suitable for therapeutic use than physostigmine.

Alzheimer Disease↗

A long-lasting cholinesterase inhibitor affecting neural and behavioral processes.

A series of analogues of physostigmine were prepared with the aim of investigating their inhibitory effects on acetylcholinesterase in the treatment of Alzheimer's disease. One of the isomers prepared was evaluated for its anticholinesterase activity in vivo, acute toxicity, and some behavioral effects. This compound was a competitive inhibitor of the enzyme and was found to antagonize the stimulating effect produced by scopolamine on locomotor activity and to facilitate memory consolidation.

Acetylcholinesterase↗

Effects of the selective kappa-opioid receptor agonist U-50,488 on locomotor activity and passive avoidance behaviour in DBA/2 and C57BL/6 mice.

Some behavioural effects of the kappa-opioid receptor agonist U-50,488 were investigated in DBA/2 (DBA) and C57BL/6 (C57) mice. In a first set of experiments, which was carried out with the toggle-floor box, U-50,488 depressed locomotor activity in both strains. Moreover, this activity depression was enhanced in both strains by the administration of haloperidol and muscimol, showing the involvement of dopaminergic and gabaergic mechanisms. In a second set of experiments, which were carried out with a passive avoidance apparatus, memory impairments, in DBA mice, and improvements, in C57 mice, were observed following immediately posttraining U-50,488 administrations. The results are compared with those of previous researches carried out, in the same strains of mice, with mu-opioid receptor agonists.

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

Strain-dependent effects of shock-induced release of opioids: dissociation between analgesia and behavioral seizures.

Intermittent, but not continuous, footshock resulted in naltrexone-reversible analgesia in two strains of mice: C57BL/6 (C57) and BALB/c (BALB). While no strain differences were evident in relation to analgesia, a clear strain effect appeared when the protective action of intermittent footshock on electroconvulsive shock-induced seizures was considered. In fact naltrexone-reversible protection exerted by intermittent footshock on behavioral seizures was much higher in C57 than in BALB mice. The reason of this dissociation between the effects of endogenous opioids on analgesia and seizures is discussed.

Analgesia↗

Human papillomavirus deoxyribonucleic acid in cervical carcinoma from primary and metastatic sites.

Tissue from 13 cervical cancers and pelvic or para-aortic lymph nodes from the same patient were evaluated by deoxyribonucleic acid hybridization with a human papillomavirus type 16 deoxyribonucleic acid probe for the presence of human papillomavirus-related deoxyribonucleic acid sequences. Twelve of the primary malignancies were squamous cancers and one was an adenocarcinoma. Eight of the primary tumors contained human papillomavirus type 16 deoxyribonucleic acid sequences, and five contained viral sequences closely related to human papillomavirus type 16. Histopathologic diagnosis confirmed malignant cells in six of 13 lymph nodes; three of these specimens contained human papillomavirus type 16 sequences while three had human papillomavirus type 16-related sequences. One lymph node that failed to show malignant cells also contained human papillomavirus type 16 deoxyribonucleic acid. The remaining lymph nodes did not contain malignant cells by either histologic examination or deoxyribonucleic acid hybridization. The human papillomavirus deoxyribonucleic acid sequences in the lymph nodes were similar to those in the matched primary cancer in all cases. These data provide further evidence implicating human papillomavirus in the etiology of cervical cancer.

Adenocarcinoma↗

Transfer of conditioning in stress-induced analgesia.

Classical conditioning of stress-induced analgesia (SIA) resulted in higher tail flick latencies in BALB/c mice. Transfer of classical conditioning of SIA was evident when the same repetition rate (pulsed light or pulsed tone) characterized stimuli in different sensory modalities. This finding is discussed in terms of opioid production and of generalization of emotional reactions.

Animals↗

Effects of flunitrazepam on passive avoidance behaviour in mice subjected to immobilization stress or familiarized with the testing apparatus.

The effects of flunitrazepam on passive avoidance behaviour were investigated in DBA/2 mice. In a first set of experiments retention performance impairment was observed in mice injected with the drug immediately but not 120 min after training. In a second set of experiments, immobilization stress enhanced, while familiarization with the apparatus decreased, the effects of flunitrazepam, suggesting involvement of emotional factors. All the effects observed were antagonized by naltrexone, showing involvement of opioid receptors.

Animals↗

A comparative study of salivary secretion by parotid and mandibular glands of anaesthetized Capra hircus: effect of pilocarpine.

A study was made of basal secretion and the effect of the infusion of pilocarpine on the flow and composition of saliva in the parotid and mandibular glands of the anaesthetized lactating goat. In the parotid gland there was a basal flow (1.6 +/- 0.29 microliter/min) which was not present in the mandibular gland. There is a statistically significant dose-effect relationship between pilocarpine and salivary flow in both glands. Salival composition and its variation with respect to the flow of saliva did not conform to either of the two glands to an exclusive monogastric or ruminant model.

Animals↗

Enhancement of morphine-induced hyperactivity by antihistaminic drugs in mice.

Three histamine H1-receptor antagonists, chlorpheniramine, diphenhydramine and tripelennamine, were tested alone or in combination with morphine on locomotor activity in C57BL/6 mice. All three antihistaminics, at some dosage levels, slightly increased activity when given alone, but strongly enhanced morphine-induced hyperactivity. The results demonstrate that locomotor activity represents a useful test to evidence stimulatory effects of antihistaminic-opiate combinations.

Animals↗

Effects of bremazocine on passive avoidance behaviour in mice.

The effects of bremazocine on memory processes were studied in DBA/2 mice tested in a passive avoidance apparatus. In a first set of experiments, memory impairments following immediately posttraining bremazocine administration (0.025 and 0.05 but not 0.01 mg/kg), and memory improvements following immediately posttraining administration of the kappa-opioid-receptor antagonist MR-1452 (1.0 and 2.0 but not 0.5 mg/kg), were observed. No effect was evident when the drugs were injected starting 120 min after training. In a second set of experiments, the effects of bremazocine (0.05 mg/kg) were antagonized by a per se ineffective dose of MR-1452 (0.5 mg/kg), suggesting involvement of kappa-opioid-receptors. In a third set of experiments, the effects of bremazocine were enhanced by a per se ineffective (15 min) immobilization stress, and were decreased by familiarization with the passive avoidance apparatus. The results are discussed in terms of attenuation of emotionality following bremazocine administration.

Analgesics↗

Diurnal variations in electroconvulsive shock-induced seizures: involvement of endogenous opioids.

Electroconvulsive shock (ECS)-induced seizures present a clear cut diurnal rhythmicity when BALB/c mice are subjected to a light-dark (L/D) schedule. On the contrary, in the absence of external synchronizers no evident fluctuations in epileptic behaviour were evident. Naloxone decreased the threshold of ECS-induced convulsions, thus confirming an involvement of opioids in this type of behaviour. These findings indicate that opioids present a diurnal (L/D) but not circadian (L/L) rhythmicity in BALB/c mice.

Adaptation, Physiological↗

Genetic differences in daily rhythms of pain sensitivity in mice.

A dark phase increase in pain sensitivity was evident in C57BL/6 inbred mice. On the contrary Swiss mice are characterized by decreased nocturnal pain sensitivity. The latter finding is in agreement with a number of previous studies based on albino mice. However, our findings indicate that (1) nocturnal decreased pain sensitivity is not the rule in the mouse and (2) large differences are evident when the onset in peak nocturnal analgesia is considered.

Animals↗

Effects of tifluadom on passive avoidance behaviour in DBA/2 mice.

The effects of the selective opiate kappa-receptor agonist tifluadom on memory were investigated in a passive avoidance task in 3 sets of experiments carried out with DBA/2 (DBA) mice both familiarized and unfamiliarized with the apparatus. In a first set of experiments, tifluadom (1.0 or 2.5, but not 0.5 mg/kg) administration immediately after training impaired retention performance of non-familiarized mice. This impairment was still evident when the drug was injected 15 or 30, but not 60 min after training. A second set of experiments was carried out with mice familiarized with the apparatus. Tifluadom was less effective in impairing memory in this group of animals, as compared with non-familiarized mice. Finally, in a third set of experiments, carried out with non-familiarized mice, a 15 min immobilization stress, which was ineffective when administered alone, enhanced the effects of tifluadom (1.0 mg/kg). The results are discussed in terms of attenuation of emotionality, resulting in impaired retention, following post-training opiate administration.

Animals↗