Opioids Flashcards
drugs that reduce pain without producing unconsciousness
narcotic analgesics
The main active ingredient in opium
morphine
Opium has other molecules like ____, ____ and ____, and the small differences in structure determine the _____ and side effects
codeine, thebaine, narcotine, effectiveness
heroin was made by adding two ____ groups to morphine, making it more _____ soluble. It reaches the brain _____, making it more ____ than morphine when injected due to increased ______. It is converted to _____ in the brain. Some opium derivatives are _______, or modified versions of opium ingredients. Other narcotics are entirely ____ and may have very different chemical structures
acetyl, lipid, faster, potent, bioavailability, morphine, semi-synthetic, synthetic
opioid receptors were first discovered using ______ binding assays, before the ____ ligands were identified. Opioid receptors are also in the ____. Selective ones were used to identify receptor subtypes: _____, ____, ____ and _____. Receptor subtypes have distinct _____ in the brain and spinal cord, suggesting they mediate a wide variety of effects. All are ____ ______ metabotropic receptors that inhibit ____ ______
radioligand, endogenous, gut, mu, delta, kappa, NOP-R, distributions, Gi protein-linked, adenylyl cyclase-cAMP
The mu receptor has a high affinity for ____, and regional distribution reflects its effects. Receptors in the medial ______, ____ ____, _____, _____, and ___ ____ mediate the analgesia. Receptors in the ____ mediate cardiovascular / respiratory control, ____ control, and nausea / vomiting. Receptors in the ___ and striatum have a role in sensorimotor integration.
morphine, thalamus, periaqueductal grey, raphe, LC, spinal cord, brainstem, cough, thalamus
mu receptors in the NAcc mediate feeding _____ _______. They mediate pleasurable aspects of ____ foods. Blocking these receptors results in reduction of ____ pleasure. Opioids are also released during _____ encounters
positive reinforcement, fatty, hedonic, sexual
the delta receptor is predominately in _____ structures. The locations suggests roles in ______, motor _____, ________ and _____ function. Reduced delta activity causes ____ in animals. A considerable number of areas overlap with ____ receptors, suggesting modulation of analgesia.
forebrain, olfaction, integration, reinforcement, cognitive, anxiety, mu
the kappa receptor are located in the _____, _____ and ______. They may participate in the regulation of _____ perception, _____ motility, and ______. They were initially identified by binding to ______
striatum, amygdala, hypothalamus, pain, gut, dysphoria, ketocyclazocine
an opioid analog that produces hallucinations and dysphoria
ketocyclazocine
Nociceptin / orphanin FQ receptors are widely distributed in the ____, ___ areas, thalamus, ___ ___ and spinal cord. The receptors are similar to other opioid receptors but do not ____ opioid drugs. Their locations suggest a role in _____, feeding, ____, ____ function, ____ and neuroendocrine regulation. Activation in the ___ _____ produces less _____ vs mu receptors but also has minimal ____ potential and causes less _____ ______. Above the spinal cord, these receptors can produce _______
cortex, limbic, raphe nuclei, bind, analgesia, learning, motor, reward, spinal cord, analgesia, abuse, respiratory depression, hyperalgesia
peptide transmitters that bind to opioid receptors were discovered in the _____ and was called _____. Multiple peptides that activate these receptors were later discovered and called _______.
1970s, enkephalin, endorphins
endogenous opioid peptides are synthesized from larger ____ peptides which are ___ into smaller peptide transmitters in the _____. These _______ contain the amino acid sequence for both endogenous opiates and other transmitters.
precursor, cleaved, terminal, propeptides
some opioid transmitters are released via long _____ projection systems, while other are released by ______ circuit neurons
axonal, local
different variants of endogenous peptides exist such as _____ or ___, met or _________. Endogenous opioid peptides are often _____ with other NTs in the nerve terminals and can be simultaneously released with ____ or ______.
dynorphin-A, B, leu-enkephalin, co-released, Glutamate, GABA
endogenous opiates are not _____ for a receptor subtype, but instead show a _____ preference. the _____ receptor is preferentially activated by endorphins and somewhat selectively activated by ______. The delta receptor is preferentially activated by ____ and _____. The Kappa receptor is preferentially activated by ______.
selective, relative, mu, endomorphins, endorphins, enkephalins, dynorphins