Benperidol
Receptors, Dopamine D2
Clonazepam
Panic Disorder
Lactation
Seizures
Imaging of striatal dopamine D(2) receptors with a PET system for small laboratory animals in comparison with storage phosphor autoradiography: a validation study with (18)F-(N-methyl)benperidol. (1/10)
Several groups have developed high-resolution PET systems and shown the feasibility of in vivo studies on small laboratory animals. In this investigation, one of these systems was validated for the performance of receptor imaging studies. For this, the radiotracer concentrations obtained in the same animals with PET and with autoradiography were quantified, and the correspondence between both methods was assessed by means of correlation analysis. METHODS: Striatal radioactivity was measured in 10 Sprague-Dawley rats after injection of 60 +/- 10 MBq of the dopamine D(2) receptor ligand (18)F-(N-methyl)benperidol in 6 time frames of 6 min each. On completion of the scans, animals were killed, and their brains were removed and sectioned using a cryostat microtome. Coronal slices were subjected to storage phosphor autoradiography with BaFBr:Eu(2+)-coated imaging plates. Striatal radioactivity was quantified in both modalities using region-of-interest analysis and activity standards. RESULTS: After partial-volume correction, the median of striatal radioactivity concentration measured with PET was 0.40 MBq/cm(3) (25th percentile, 0.32; 75th percentile, 0.44). Radioactivity concentrations determined by means of storage phosphor autoradiography amounted to 0.42 MBq/cm(3) (25th percentile, 0.24; 75th percentile, 0.51). Correlation of striatal radioactivity values yielded a Pearson correlation coefficient of 0.818 (P = 0.002). Radioactivity accumulation in Harder's glands led to an overestimation of striatal activity concentrations by approximately 5%. The median of striatal radioactivity concentration after spillover correction decreased slightly to 0.38 MBq/cm(3) (25th percentile, 0.30; 75th percentile, 0.43). Correlation of striatal radioactivity values after spillover correction yielded a Pearson correlation coefficient of 0.824 (P = 0.002). CONCLUSION: The results show a significant positive correlation between radioactivity values obtained with PET and storage phosphor autoradiography used as the gold standard. Because we applied a selective dopamine D(2) receptor radioligand and because radioactivity concentrations could be reliably quantified in the target region, we may infer that in vivo receptor binding studies will be possible in small laboratory animals. (+info)In vivo measurement of D2 receptor density and affinity for 18F-(3-N-methyl)benperidol in the rat striatum with a PET system for small laboratory animals. (2/10)
A recent investigation showed that intracerebral radioactivity concentrations can reliably be quantified in vivo with a small-animal PET device. The purpose of the current study was to investigate the binding characteristics of the D(2) receptor radioligand (18)F-(3-N-methyl)benperidol ((18)FMB) in rat striatum by determining receptor density (B(max)) and affinity (K(d)) in vivo. For validation, K(d) and B(max) additionally were determined in vitro using storage phosphor autoradiography. METHODS: Striatal radioactivity was measured with PET in 8 Sprague-Dawley rats after injection of (18)FMB in increasing specific activities. Free radioligand concentrations were estimated from cortical radioactivity concentrations and were subtracted from striatal radioactivity concentrations to obtain specific binding. In vitro saturation experiments were performed on 7 further rats according to the isotopic dilution method. Specific binding was determined by both subtraction of (18)FMB binding in the presence of raclopride and subtraction of cortical radioactivity concentrations from total radioligand binding. Saturation binding curves were obtained by plotting specifically bound radioligand concentrations against free radioligand concentrations and were evaluated with regression analysis. RESULTS: PET yielded a K(d) of 6.2 nmol/L and a B(max) of 16 fmol/mg for the striatal D(2) receptor. In vitro, K(d) and B(max) amounted to 4.4 nmol/L and 84.1 fmol/mg (subtraction of (18)FMB binding in the presence of raclopride), respectively, and 7.9 nmol/L and 70.1 fmol/mg (subtraction of cortical radioactivity concentrations), respectively. CONCLUSION: K(d) values measured with PET and autoradiography agreed and corresponded to inhibition constants obtained in previous in vitro studies. B(max) values lay within the same order of magnitude. The results of in vitro saturation binding analyses also agreed, irrespective of the mode of determination of free radioligand concentrations. Thus, B(max) and K(d) may be determined with PET in analogy to the evaluation of in vitro binding data by regression analysis of bound-versus-free ligand concentrations. Our results show that small-animal tomographs are valuable tools for the in vivo characterization of receptor radioligands as an alternative to autoradiography. (+info)Radiation dosimetry of N-([11C]methyl)benperidol as determined by whole-body PET imaging of primates. (3/10)
PURPOSE: N-([(11)C]methyl)benperidol ([(11)C]NMB) can be used for positron emission tomography (PET) measurements of D(2)-like dopamine receptor binding in vivo. We report the absorbed radiation dosimetry of i.v.-administered (11)C-NMB, a critical step before applying this radioligand to imaging studies in humans. MATERIALS AND METHODS: Whole-body PET imaging with a CTI/Siemens ECAT 953B scanner was done in a male and a female baboon. After i.v. injection of 444-1221 MBq of (11)C-NMB, sequential images taken from the head to the pelvis were collected for 3 h. Volumes of interest (VOIs) were identified that entirely encompassed small organs (whole brain, striatum, eyes, and myocardium). Large organs (liver, lungs, kidneys, lower large intestine, and urinary bladder) were sampled by drawing representative regions within the organ volume. Time-activity curves for each VOI were extracted from the PET, and organ residence times were calculated by analytical integration of a multi-exponential fit of the time-activity curves. Human radiation doses were estimated using OLINDA/EXM 1.0 and the standard human model. RESULTS: Highest retention was observed in the blood and liver, each with total residence times of 1.5 min. The highest absorbed radiation doses were to the heart (10.5 muGy/MBq) [DOSAGE ERROR CORRECTED] and kidney (9.19 muGy/MBq), [DOSAGE ERROR CORRECTED] making these the critical organs for [(11)C]NMB. A heart absorption of 50 mGy would result from an injected dose of 4,762 MBq [(11)C]NMB. CONCLUSIONS: Thus, this study suggests that up to 4,762 MBq of [(11)C]NMB can be safely administered to human subjects for PET studies. Total body dose and effective dose for [(11)C]NMB are 2.82 muGy/MBq [DOSAGE ERROR CORRECTED] and 3.7 mSv/kBq, respectively. (+info)Validation of the reference tissue model for estimation of dopaminergic D2-like receptor binding with [18F](N-methyl)benperidol in humans. (4/10)
(+info)In vivo labeling of the dopamine D2 receptor with N-11C-methyl-benperidol. (5/10)
A new dopamine D2 receptor radiotracer, N-11C-methyl-benperidol (11C-NMB), was prepared and its in vivo biologic behavior in mice and a baboon was studied. Carbon-11-NMB was determined to bind to specific sites characterized as dopamine D2 receptors. The binding was saturable, reversible, and stereospecific. Kinetic studies in the dopamine D2 receptor-rich striatum showed that 11C-NMB was retained five times longer than in receptor-devoid regions, resulting in a high maximum striatal-to-cerebellar ratio of 11:1 at 60 min after injection. From frontal cortex and cortex, on the other hand, the tracer washed out as rapidly as it did from cerebellum, resulting in tissue-to-cerebellar ratios close to one in these regions at any time after injection. Blocking studies confirmed the specificity and selectivity of the 11C-NMB binding to the dopamine D2 receptor. A PET study with 11C-NMB of the baboon brain revealed highly selective labeling of dopamine D2 receptor sites which was blocked by preinjection of raclopride. (+info)Characterization of extrastriatal D2 in vivo specific binding of [(1)(8)F](N-methyl)benperidol using PET. (6/10)
(+info)Syntheses and specific activity determinations of no-carrier-added (NCA) F-18-labeled butyrophenone neuroleptics--benperidol, haloperidol, spiroperidol, and pipamperone. (7/10)
A general method for the syntheses of no-carrier-added (NCA) 18F-labeled butyrophenone neuroleptics--benperidol, haloperidol, spiroperidol, and pipamperone is described. These 18F-labeled neuroleptic drugs are synthesized by a multistep synthesis in an overall radiochemical yield of 10-20% at end of bombardment (EOB) in a synthesis time of 90 min from EOB. The sequence involves the synthesis of NCA p-[18F]fluorobenzonitrile from NCA [18F]-fluoride and p-nitrobenzonitrile using the rapidly converted to gamma-chloro-p-[18F]fluorobutyrophenone which is alkylated with appropriate amines to give NCA 18F-labeled benperidol, haloperidol, spiroperidol, and pipamperone. The final product is purified by preparative high performance liquid chromatography (HPLC). The 18F solution used in the synthesis as determined by ion chromatography contains 15.3 +/- 9.0 nmol of stable fluoride. The specific activities of the resulting butyrophenone neuroleptics were determined to be 3 Ci/mumol (at EOB) (range 1-6 Ci/mumol) as determined by radioreceptor assay and HPLC assay. (+info)A comparative study of conventional premedication (pethidine, promethazine, and atropine) and neuroleptanalgesia (droperidol and phenoperidine) for peroral endoscopy. (8/10)
A double blind comparison of conventional premedication (pethidine, promethazine, and atropine) and neuroleptanalgesia (droperidol and phenoperidine) failed to demonstrate any difference in either the comfort of the patient or ease of instrumentation in 70 upper gastrointestinal tract endoscopies. Further trials are needed before conventional premedication is abandoned. (+info)Benperidol is a butyrophenone derivative that is primarily used as an antipsychotic medication. Its medical definition can be broken down into its chemical class, mechanism of action, and clinical uses.
Chemical Class: Benperidol belongs to the chemical class of butyrophenones, which are a group of synthetic compounds with diverse pharmacological activities, including antipsychotic, antiemetic, and sedative effects.
Mechanism of Action: Benperidol works by blocking dopamine receptors in the brain, particularly the D2 receptor subtype. Dopamine is a neurotransmitter that plays a crucial role in regulating movement, emotion, and cognition. By blocking dopamine receptors, benperidol reduces the amount of dopamine available to stimulate these receptors, which can help alleviate symptoms of psychosis, such as hallucinations, delusions, and disorganized thinking.
Clinical Uses: Benperidol is primarily used to treat chronic schizophrenia and other related psychotic disorders. It may also be used off-label for the management of severe aggression or agitation in individuals with developmental disabilities or dementia. However, its use is limited due to its significant side effects, including extrapyramidal symptoms (EPS), such as rigidity, tremors, and involuntary movements, and potential for causing tardive dyskinesia, a neurological disorder characterized by involuntary movements of the face, tongue, or limbs.
It is important to note that benperidol should only be prescribed and administered under the supervision of a qualified healthcare professional, as its use requires careful monitoring and management of potential side effects.
Dopamine D2 receptor is a type of metabotropic G protein-coupled receptor that binds to the neurotransmitter dopamine. It is one of five subtypes of dopamine receptors (D1-D5) and is encoded by the gene DRD2. The activation of D2 receptors leads to a decrease in the activity of adenylyl cyclase, which results in reduced levels of cAMP and modulation of ion channels.
D2 receptors are widely distributed throughout the central nervous system (CNS) and play important roles in various physiological functions, including motor control, reward processing, emotion regulation, and cognition. They are also involved in several neurological and psychiatric disorders, such as Parkinson's disease, schizophrenia, drug addiction, and Tourette syndrome.
D2 receptors have two main subtypes: D2 short (D2S) and D2 long (D2L). The D2S subtype is primarily located in the presynaptic terminals and functions as an autoreceptor that regulates dopamine release, while the D2L subtype is mainly found in the postsynaptic neurons and modulates intracellular signaling pathways.
Antipsychotic drugs, which are used to treat schizophrenia and other psychiatric disorders, work by blocking D2 receptors. However, excessive blockade of these receptors can lead to side effects such as extrapyramidal symptoms (EPS), tardive dyskinesia, and hyperprolactinemia. Therefore, the development of drugs that selectively target specific subtypes of dopamine receptors is an active area of research in the field of neuropsychopharmacology.
Clonazepam is a medication that belongs to a class of drugs called benzodiazepines. It is primarily used to treat seizure disorders, panic attacks, and anxiety. Clonazepam works by increasing the activity of gamma-aminobutyric acid (GABA), a neurotransmitter in the brain that has a calming effect on the nervous system.
The medication comes in tablet or orally disintegrating tablet form and is typically taken two to three times per day. Common side effects of clonazepam include dizziness, drowsiness, and coordination problems. It can also cause memory problems, mental confusion, and depression.
Like all benzodiazepines, clonazepam has the potential for abuse and addiction, so it should be used with caution and only under the supervision of a healthcare provider. It is important to follow the dosage instructions carefully and not to stop taking the medication suddenly, as this can lead to withdrawal symptoms.
It's important to note that while I strive to provide accurate information, this definition is intended to be a general overview and should not replace professional medical advice. Always consult with a healthcare provider for medical advice.
Anxiety disorders are a category of mental health disorders characterized by feelings of excessive and persistent worry, fear, or anxiety that interfere with daily activities. They include several different types of disorders, such as:
1. Generalized Anxiety Disorder (GAD): This is characterized by chronic and exaggerated worry and tension, even when there is little or nothing to provoke it.
2. Panic Disorder: This is characterized by recurring unexpected panic attacks and fear of experiencing more panic attacks.
3. Social Anxiety Disorder (SAD): Also known as social phobia, this is characterized by excessive fear, anxiety, or avoidance of social situations due to feelings of embarrassment, self-consciousness, and concern about being judged or viewed negatively by others.
4. Phobias: These are intense, irrational fears of certain objects, places, or situations. When a person with a phobia encounters the object or situation they fear, they may experience panic attacks or other severe anxiety responses.
5. Agoraphobia: This is a fear of being in places where it may be difficult to escape or get help if one has a panic attack or other embarrassing or incapacitating symptoms.
6. Separation Anxiety Disorder (SAD): This is characterized by excessive anxiety about separation from home or from people to whom the individual has a strong emotional attachment (such as a parent, sibling, or partner).
7. Selective Mutism: This is a disorder where a child becomes mute in certain situations, such as at school, but can speak normally at home or with close family members.
These disorders are treatable with a combination of medication and psychotherapy (cognitive-behavioral therapy, exposure therapy). It's important to seek professional help if you suspect that you or someone you know may have an anxiety disorder.
I'm sorry for any confusion, but "Economics, Nursing" is not a standard medical or nursing term or concept. Economics is the social science that deals with the production, distribution, and consumption of goods and services, while nursing is a field of healthcare concerned with the care of individuals, families, and communities to achieve, maintain, or recover optimal health and quality of life.
If you're looking for information on how economics intersects with nursing or healthcare more broadly, there is a subfield of study known as "health economics" that examines issues related to the financing, delivery, and consumption of healthcare resources. However, I would need more context to provide a more specific definition or explanation.
Panic Disorder is a type of anxiety disorder characterized by recurrent, unexpected panic attacks and significant worry about the implications of these attacks or fear of their occurrence. A panic attack is a sudden surge of intense fear or discomfort that reaches a peak within minutes, and includes physical symptoms such as accelerated heart rate, sweating, trembling, shortness of breath, and feelings of impending doom or danger. In Panic Disorder, these attacks are not triggered by specific situations or stimuli, but can occur spontaneously and without warning. The individual may also develop avoidance behaviors to prevent future panic attacks, which can interfere with daily functioning and quality of life.
Lactation is the process by which milk is produced and secreted from the mammary glands of female mammals, including humans, for the nourishment of their young. This physiological function is initiated during pregnancy and continues until it is deliberately stopped or weaned off. The primary purpose of lactation is to provide essential nutrients, antibodies, and other bioactive components that support the growth, development, and immune system of newborns and infants.
The process of lactation involves several hormonal and physiological changes in a woman's body. During pregnancy, the hormones estrogen and progesterone stimulate the growth and development of the mammary glands. After childbirth, the levels of these hormones drop significantly, allowing another hormone called prolactin to take over. Prolactin is responsible for triggering the production of milk in the alveoli, which are tiny sacs within the breast tissue.
Another hormone, oxytocin, plays a crucial role in the release or "let-down" of milk from the alveoli to the nipple during lactation. This reflex is initiated by suckling or thinking about the baby, which sends signals to the brain to release oxytocin. The released oxytocin then binds to receptors in the mammary glands, causing the smooth muscles around the alveoli to contract and push out the milk through the ducts and into the nipple.
Lactation is a complex and highly regulated process that ensures the optimal growth and development of newborns and infants. It provides not only essential nutrients but also various bioactive components, such as immunoglobulins, enzymes, and growth factors, which protect the infant from infections and support their immune system.
In summary, lactation is the physiological process by which milk is produced and secreted from the mammary glands of female mammals for the nourishment of their young. It involves hormonal changes, including the actions of prolactin, oxytocin, estrogen, and progesterone, to regulate the production, storage, and release of milk.
A seizure is an uncontrolled, abnormal firing of neurons (brain cells) that can cause various symptoms such as convulsions, loss of consciousness, altered awareness, or changes in behavior. Seizures can be caused by a variety of factors including epilepsy, brain injury, infection, toxic substances, or genetic disorders. They can also occur without any identifiable cause, known as idiopathic seizures. Seizures are a medical emergency and require immediate attention.
An algorithm is not a medical term, but rather a concept from computer science and mathematics. In the context of medicine, algorithms are often used to describe step-by-step procedures for diagnosing or managing medical conditions. These procedures typically involve a series of rules or decision points that help healthcare professionals make informed decisions about patient care.
For example, an algorithm for diagnosing a particular type of heart disease might involve taking a patient's medical history, performing a physical exam, ordering certain diagnostic tests, and interpreting the results in a specific way. By following this algorithm, healthcare professionals can ensure that they are using a consistent and evidence-based approach to making a diagnosis.
Algorithms can also be used to guide treatment decisions. For instance, an algorithm for managing diabetes might involve setting target blood sugar levels, recommending certain medications or lifestyle changes based on the patient's individual needs, and monitoring the patient's response to treatment over time.
Overall, algorithms are valuable tools in medicine because they help standardize clinical decision-making and ensure that patients receive high-quality care based on the latest scientific evidence.
Benperidol
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Anquil1
- Benperidol, sold under the trade name Anquil among others, is a typical antipsychotic primarily used to treat hypersexuality syndromes and can be used to treat schizophrenia. (wikipedia.org)
Haloperidol1
- Benperidol is a butyrophenone antipsychotic, with general properties similar to those of haloperidol . (guidetopharmacology.org)
Antipsychotic1
- The atypical antipsychotic risperidone , although not a butyrophenone, was developed with the structures of benperidol and lenperone as a basis. (wikidoc.org)
Dopamine1
- Objective: To investigate the associations between manganese (Mn) exposure, D2 dopamine receptors (D2Rs), and parkinsonism using [11C](N-methyl)benperidol (NMB) PET. (cdc.gov)
Drug2
- Benperidol - a drug for sexual offenders? (wikipedia.org)
- New evidence for memantine and benperidol (including a thorough QT study, review of case reports, and drug label changes) does not indicate that memantine or benperidol are associated with QT prolongation under normal conditions of use. (crediblemeds.org)
Decreases1
- Use using is has (4)benperidol directed and albuterol decreases. (lennimattanja.com)
Patients2
- Benperidol should be used with caution in patients with risk factors for stroke. (medthority.com)
- Table un una side in en ipratropium Patients cause efficacy que such inhalado, Ventolin Best Price , in lung Tiotropium sore tratamientos chest con de that to terapéuticamente tract irritation leg la. (lennimattanja.com)
Properties1
- Benperidol is a butyrophenone antipsychotic, with general properties similar to those of haloperidol . (guidetopharmacology.org)