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Opioid Receptors
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain, in the spinal cord, on peripheral neurons, and digestive tract. Discovery By the mid-1960s, it had become apparent from pharmacologic studies that opiate drugs were likely to exert their actions at specific receptor sites, and that there were likely to be multiple such sites. Early studies had indicated that opiates appeared to accumulate in the brain. The receptors were first identified as specific molecules through the use of binding studies, in which opiates that had been labeled with radioisotopes were found to bind to brain membrane homogenates. The first such study was published in 1971, using 3H-levorphanol. In 1973, Candace Pert and Solomon H. Snyder publis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tritium
Tritium ( or , ) or hydrogen-3 (symbol T or H) is a rare and radioactive isotope of hydrogen with half-life about 12 years. The nucleus of tritium (t, sometimes called a ''triton'') contains one proton and two neutrons, whereas the nucleus of the common isotope hydrogen-1 (''protium'') contains one proton and zero neutrons, and that of hydrogen-2 (''deuterium'') contains one proton and one neutron. Naturally occurring tritium is extremely rare on Earth. The atmosphere has only trace amounts, formed by the interaction of its gases with cosmic rays. It can be produced artificially by irradiating lithium metal or lithium-bearing ceramic pebbles in a nuclear reactor and is a low-abundance byproduct in normal operations of nuclear reactors. Tritium is used as the energy source in radioluminescent lights for watches, gun sights, numerous instruments and tools, and even novelty items such as self-illuminating key chains. It is used in a medical and scientific setting as a radioacti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sensory Neurons
Sensory neurons, also known as afferent neurons, are neurons in the nervous system, that convert a specific type of stimulus, via their receptors, into action potentials or graded potentials. This process is called sensory transduction. The cell bodies of the sensory neurons are located in the dorsal ganglia of the spinal cord. The sensory information travels on the afferent nerve fibers in a sensory nerve, to the brain via the spinal cord. The stimulus can come from ''exteroreceptors'' outside the body, for example those that detect light and sound, or from ''interoreceptors'' inside the body, for example those that are responsive to blood pressure or the sense of body position. Types and function Different types of sensory neurons have different sensory receptors that respond to different kinds of stimuli. There are at least six external and two internal sensory receptors: External receptors External receptors that respond to stimuli from outside the body are called ex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerebral Cortex
The cerebral cortex, also known as the cerebral mantle, is the outer layer of neural tissue of the cerebrum of the brain in humans and other mammals. The cerebral cortex mostly consists of the six-layered neocortex, with just 10% consisting of allocortex. It is separated into two cortices, by the longitudinal fissure that divides the cerebrum into the left and right cerebral hemispheres. The two hemispheres are joined beneath the cortex by the corpus callosum. The cerebral cortex is the largest site of neural integration in the central nervous system. It plays a key role in attention, perception, awareness, thought, memory, language, and consciousness. The cerebral cortex is part of the brain responsible for cognition. In most mammals, apart from small mammals that have small brains, the cerebral cortex is folded, providing a greater surface area in the confined volume of the cranium. Apart from minimising brain and cranial volume, cortical folding is crucial for the brain ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olfactory Bulbs
The olfactory bulb (Latin: ''bulbus olfactorius'') is a neural structure of the vertebrate forebrain involved in olfaction, the sense of smell. It sends olfactory information to be further processed in the amygdala, the orbitofrontal cortex (OFC) and the hippocampus where it plays a role in emotion, memory and learning. The bulb is divided into two distinct structures: the main olfactory bulb and the accessory olfactory bulb. The main olfactory bulb connects to the amygdala via the piriform cortex of the primary olfactory cortex and directly projects from the main olfactory bulb to specific amygdala areas. The accessory olfactory bulb resides on the dorsal-posterior region of the main olfactory bulb and forms a parallel pathway. Destruction of the olfactory bulb results in ipsilateral anosmia, while irritative lesions of the uncus can result in olfactory and gustatory hallucinations. Structure In most vertebrates, the olfactory bulb is the most rostral (forward) part of the br ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amygdala
The amygdala (; plural: amygdalae or amygdalas; also '; Latin from Greek, , ', 'almond', 'tonsil') is one of two almond-shaped clusters of nuclei located deep and medially within the temporal lobes of the brain's cerebrum in complex vertebrates, including humans. Shown to perform a primary role in the processing of memory, decision making, and emotional responses (including fear, anxiety, and aggression), the amygdalae are considered part of the limbic system. The term "amygdala" was first introduced by Karl Friedrich Burdach in 1822. Structure The regions described as amygdala nuclei encompass several structures of the cerebrum with distinct connectional and functional characteristics in humans and other animals. Among these nuclei are the basolateral complex, the cortical nucleus, the medial nucleus, the central nucleus, and the intercalated cell clusters. The basolateral complex can be further subdivided into the lateral, the basal, and the accessory basal nucle ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pons
The pons (from Latin , "bridge") is part of the brainstem that in humans and other bipeds lies inferior to the midbrain, superior to the medulla oblongata and anterior to the cerebellum. The pons is also called the pons Varolii ("bridge of Varolius"), after the Italian anatomist and surgeon Costanzo Varolio (1543–75). This region of the brainstem includes neural pathways and tracts that conduct signals from the brain down to the cerebellum and medulla, and tracts that carry the sensory signals up into the thalamus.Saladin Kenneth S.(2007) Anatomy & physiology the unity of form and function. Dubuque, IA: McGraw-Hill Structure The pons is in the brainstem situated between the midbrain and the medulla oblongata, and in front of the cerebellum. A separating groove between the pons and the medulla is the inferior pontine sulcus. The superior pontine sulcus separates the pons from the midbrain. The pons can be broadly divided into two parts: the basilar part of the pons (ventral ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
δ-opioid Receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands. The regions of the brain where the δ-opioid receptor is largely expressed vary from species model to species model. In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain. Function The endogenous system of opioid receptors is well known for its analgesic potential; however, the exact role of δ-opioid receptor activation in pain modulation is largely up for debate. This also depends on the model at hand since receptor activity is known to change from species to species. Activation of delta receptors produces analgesia, perhaps as significant potentiators of μ-opioid receptor agonists. However, it seems like delta agonism provides heavy potentiation to any mu agonism. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlornaltrexamine
Chlornaltrexamine is an irreversible mixed agonist–antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine. Its alkylating group is a bis(chloroalkyl)amino-residue similar to that of the nitrogen mustards. See also * Chloroxymorphamine, an irreversible full agonist * Naloxazone, an irreversible μ-opioid antagonist * Oxymorphazone Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound. This g ..., an irreversible full agonist References Alkylating agents Organochlorides Semisynthetic opioids Phenols 4,5-Epoxymorphinans Irreversible agonists Nitrogen mustards Chloroethyl compounds Cyclopropyl compounds {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Naloxone
Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter decreased breathing in opioid overdose. Effects begin within two minutes when given intravenously, and within five minutes when injected into a muscle. The medicine can also be administered by spraying it into a person's nose. Naloxone commonly blocks the effects of opioids for 30 to 90 minutes. Multiple doses may be required, as the duration of action of some opioids is greater than that of naloxone. Administration to opioid-dependent individuals may cause symptoms of opioid withdrawal, including restlessness, agitation, nausea, vomiting, a fast heart rate, and sweating. To prevent this, small doses every few minutes can be given until the desired effect is reached. In those with previous heart disease or taking medications that negatively affect the heart, further heart problems have occurred. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Μ-opioid Receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, inhibiting adenylate cyclase activity, lowering cAMP levels. Structure The structure of the μ-opioid receptor has been determined with the antagonist β-FNA, the agonist BU72, and in a complex with DAMGO and Gi protein. Splice variants Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. Location They can exist either presynaptically or postsynaptically depending upon cell types. The μ-opioid receptors exist mostly presynaptically in the periaqueductal gray region, and in the superfi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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