Five adult cats received four doses of phencyclidine to determine the behavioral effects of this compound. On alternate weeks the animals received control injections of saline vehicle. Dose-dependent behavioral changes occurred in three general categories (posture, locomotor activity and stereotyped head movements). In small doses (0.1 and 0.5 mg/kg), major postural effects consisted of head and body tremors and loss of hindlimb support. In larger doses (1.0 and 2.0 mg/kg), the postural effects occurred more rapidly and became more severe as animals lost both forelimb and hindlimb support and ultimately became immobile. Small doses of phencyclidine produced decreases in locomotor activity, followed by increases. Larger doses produced initial increases in activity. Increases in head movement stereotypies were produced by all doses of phencyclidine.
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http://dx.doi.org/10.1016/0028-3908(85)90152-2 | DOI Listing |
Cureus
November 2023
Surgical Critical Care, Sanford Medical Center, Fargo, USA.
Ketamine is a phencyclidine (PCP) derivative, which primarily acts as a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. Ketamine serves as an analgesic and a dissociative sedative that produces potent analgesia, sedation, and amnesia while preserving spontaneous respiratory drive. It is rapidly gaining acceptance in the management of pain as multiple studies have demonstrated its reliable efficacy and a wide margin of safety.
View Article and Find Full Text PDFBr J Pharmacol
April 2024
Sage Therapeutics Inc, Cambridge, Massachusetts, USA.
Background And Purpose: Select neuroactive steroids tune neural activity by modulating excitatory and inhibitory neurotransmission, including the endogenous cholesterol metabolite 24(S)-hydroxycholesterol (24(S)-HC), which is an N-methyl-d-aspartate (NMDA) receptor positive allosteric modulator (PAM). NMDA receptor PAMs are potentially an effective pharmacotherapeutic strategy to treat conditions associated with NMDA receptor hypofunction.
Experimental Approach: Using in vitro and in vivo electrophysiological recording experiments and behavioural approaches, we evaluated the effect of SAGE-718, a novel neuroactive steroid NMDA receptor PAM currently in clinical development for the treatment of cognitive impairment, on NMDA receptor function and endpoints that are altered by NMDA receptor hypoactivity and assessed its safety profile.
Eur J Pharmacol
August 2023
Department of Neuroscience and Experimental Therapeutics, CSIC-Institut d'Investigacions Biomèdiques de Barcelona, Barcelona, Spain; Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), Barcelona, Spain; Centro de Investigación Biomédica en Red de Salud Mental (CIBERSAM), Instituto de Salud Carlos III, Madrid, Spain.
Antipsychotic drugs of different chemical/pharmacological families show preferential dopamine (DA) D receptor (D-R) vs. D receptor (D-R) affinity, with the exception of clozapine, the gold standard of schizophrenia treatment, which shows a comparable affinity for both DA receptors. Here, we examined the ability of Lu AF35700 (preferential D-R>D-R antagonist), to reverse the alterations in thalamo-cortical activity induced by phencyclidine (PCP), used as a pharmacological model of schizophrenia.
View Article and Find Full Text PDFACS Chem Neurosci
June 2023
Department of Pharmaceutical Sciences, Union University College of Pharmacy, Jackson, Tennessee 38305, United States.
Dextromethorphan (DXM) was introduced in 1958 as the first non-opioid cough suppressant and is indicated for multiple psychiatric disorders. It has been the most used over-the-counter cough suppressant since its emergence. However, individuals quickly noticed an intoxicating and psychedelic effect if they ingested large doses.
View Article and Find Full Text PDFBiochem Biophys Res Commun
July 2023
Department of Psychiatry and Behavioral Science, Seoul National University College of Medicine, Seoul, Republic of Korea; Institute of Human Behavioral Medicine, Medical Research Center, Seoul National University, Republic of Korea. Electronic address:
Repeated administration of drugs of abuse leads to progressively greater behavioral responses; this phenomenon is referred to as behavioral sensitization. MK-801 blocks the N-methyl-d-aspartate (NMDA) receptor and elicits behavioral sensitization. Ketamine and phencyclidine, are also NMDA antagonists and have well-documented abuse potential.
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