Wakefulness-Promoting Agents
Receptors, Adrenergic, alpha-2
Interleukin 1 Receptor Antagonist Protein
Neurokinin-1 Receptor Antagonists
Purinergic P1 Receptor Antagonists
Dose-Response Relationship, Drug
Rats, Sprague-Dawley
Histamine H2 Antagonists
Serotonin 5-HT3 Receptor Antagonists
Excitatory Amino Acid Antagonists
Angiotensin Receptor Antagonists
Dopamine Antagonists
Serotonin 5-HT2 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Hormone Antagonists
Adenosine A1 Receptor Antagonists
Purinergic P2 Receptor Antagonists
Rats, Wistar
Histamine H1 Antagonists
Receptors, Endothelin
Muscarinic Antagonists
GABA-A Receptor Antagonists
Adrenergic alpha-1 Receptor Antagonists
Serotonin Antagonists
GABA Antagonists
Sialoglycoproteins
Histamine Antagonists
Receptors, Adrenergic, alpha
alpha 1-Antitrypsin
Leukotriene Antagonists
Receptor, Endothelin A
Receptors, Serotonin
Receptors, N-Methyl-D-Aspartate
Serotonin 5-HT1 Receptor Antagonists
Nicotinic Antagonists
Dizocilpine Maleate
Receptors, Interleukin-1
Adrenergic alpha-2 Receptor Antagonists
Adrenergic alpha-Antagonists
Biphenyl Compounds
Tetrazoles
Radioligand Assay
Pyridines
Guinea Pigs
Serotonin Receptor Agonists
Peptides, Cyclic
Drug Interactions
Indoles
Histamine H3 Antagonists
Binding, Competitive
Pyrazoles
Hypoxia-Inducible Factor 1, alpha Subunit
Quinoxalines
Cells, Cultured
Losartan
Endothelin-1
GABA-B Receptor Antagonists
Substance P
alpha7 Nicotinic Acetylcholine Receptor
Serotonin
Receptors, Bradykinin
Signal Transduction
Neurons
Cimetidine
Receptors, Neurokinin-1
Adenosine A3 Receptor Antagonists
Receptor, Endothelin B
Purinergic P2X Receptor Antagonists
Piperazines
Pyrrolidines
Receptors, Adrenergic, alpha-1
Interleukin-1
Receptors, Cholecystokinin
Devazepide
Adrenergic Antagonists
Prazosin
Receptors, Thromboxane
Receptors, Vasopressin
Ketanserin
2-Amino-5-phosphonovalerate
Serotonin 5-HT4 Receptor Antagonists
Disease Models, Animal
Receptor, Cannabinoid, CB1
Mice, Inbred C57BL
Receptors, Dopamine D2
Adenosine
Naltrexone
Famotidine
Receptors, Neurokinin-2
Calcium
Bradykinin
Cannabinoid Receptor Antagonists
Naloxone
Quinuclidines
Benzodiazepinones
Histamine
Adrenergic beta-2 Receptor Antagonists
Bicuculline
Receptors, Nicotinic
Imidazoles
Interleukin-1alpha
Mineralocorticoid Receptor Antagonists
Receptors, Histamine H3
Yohimbine
Receptors, Opioid
Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/222)
The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors. (+info)G-protein activation by putative antagonists at mutant Thr373Lys alpha2A adrenergic receptors. (2/222)
1. Replacement of a threonine by a lysine at position 373 in the C-terminal portion of the third intracellular loop of the human alpha2A-adrenergic receptor (alpha2A AR) has been reported to generate a constitutively active mutant receptor in analogy with similar mutations in the alpha1B and beta2 AR (Ren et al., 1993). In the present study, the mutant Thr373Lys alpha2A AR receptor was investigated by measuring the formation of inositol phosphates in either the absence or presence of mouse G(alpha)15 protein in Cos-7 cells. 2. Increased affinity, potency and/or efficacy for the agonists [(-)-adrenaline, UK 14304, clonidine, guanabenz and oxymetazoline] was observed, consistent with a precoupled mutant alpha2A AR: G-protein state. The basal inositol phosphates response was similar at the wild-type (wt) and mutant alpha2A AR, but was enhanced at the mutant alpha2A AR upon co-expression with the mouse G(alpha)15 protein. This enhanced response could not be attenuated in the presence of any of the tested alpha2 AR antagonists (10 microM), suggesting that inverse agonist activity did not occur at the mutant alpha2A AR. 3. Ligands that so far have been identified as antagonists at the wt alpha2A AR demonstrated either no intrinsic activity (MK 912, WB 4101, RS 15385, RX 811059 and RX 821002) or positive efficacy [Emax, % vs. 1 microM UK 14304: dexefaroxan (27+/-7), idazoxan (34+/-9), atipamezole (27+/-4), BRL 44408 (59+/-5) and SKF 86466 (54+/-9)] at the mutant alpha2A AR, but only in the presence of the mouse G(alpha)15 protein. The ligand potencies corresponded with their respective pKi values at the mutant alpha2A AR receptor. 4. The partial agonist effect of SKF 86466 was resistant to pertussis toxin treatment (100 ng ml(-1)) and not affected by co-expression of the rat G(alpha)i1 protein. It was virtually absent in the presence of 10 microM RS 15385. SKF 86466 was without intrinsic activity upon co-expression of the mouse G(alpha)q protein. 5. Some putative alpha2 AR antagonists exerted a partial agonist activity that was highly dependent on the presence of specific G-protein alpha-subunits, suggesting that these ligands cause selective G-protein activation at the mutant alpha2A AR. (+info)Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/222)
The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory. (+info)Effects of GABA on noradrenaline release and vasoconstriction induced by renal nerve stimulation in isolated perfused rat kidney. (4/222)
We examined effects of gamma-aminobutyric acid (GABA) on vasoconstriction and noradrenaline (NA) release induced by electrical renal nerve stimulation (RNS) in the isolated pump-perfused rat kidney. RNS (1 and 2 Hz for 2.5 min each, 0.5-ms duration, supramaximal voltage) increased renal perfusion pressure (PP) and renal NA efflux. GABA (3, 10 and 100 microM) attenuated the RNS-induced increases in PP by 10-40% (P<0.01) and NA efflux by 10-30% (P<0.01). GABA did not affect exogenous NA (40 and 60 nM)-induced increases in PP. The selective GABA(B) agonist baclofen (3, 10 and 100 microM) also attenuated the RNS-induced increases in PP and NA efflux, whereas the RNS-induced responses were relatively resistant to the selective GABA(A) agonist muscimol (3, 10 and 100 microM). The selective GABA(B) antagonist 2-hydroxysaclofen (50 microM), but not the selective GABA(A) antagonist bicuculline (50 microM), abolished the inhibitory effects of GABA (10 microM) on the RNS-induced responses. The selective alpha2-adrenoceptor antagonist rauwolscine (10 nM) enhanced the RNS-induced responses. GABA (3, 10 and 100 microM) potently attenuated the RNS-induced increases in PP by 40-60% (P<0.01) and NA efflux by 20-50% (P<0.01) in the presence of rauwolscine. Prazosin (10 and 30 nM) suppressed the RNS-induced increases in PP by about 70-80%. Neither rauwolscine (10 nM) nor GABA (10 microM) suppressed the residual prazosin-resistant PP response. These results suggest that GABA suppresses sympathetic neurotransmitter release via presynaptic GABA(B) receptors, and thereby attenuates adrenergically induced vasoconstriction in the rat kidney. (+info)Blocking effects of phentolamine on L-type calcium current and ATP-sensitive potassium current in guinea pig ventricular myocytes. (5/222)
AIM: To study the effect of phentolamine on L-type calcium currents (ICa) and ATP-sensitive K+ currents (IK,ATP) in ventricular myocytes. METHODS: ICa and IK,ATP were observed using patch clamp techniques in whole-cell recording configuration. RESULTS: Phentolamine reduced ICa of ventricular myocytes in concentration-dependent and voltage-independent manners. Phentolamine 5, 25, and 100 mumol.L-1 decreased ICa from 370 +/- 99 nA to 310 +/- 95 nA (17% block, n = 6, P < 0.01), from 230 +/- 98 nA to 180 +/- 73 nA (23% block, n = 5, P < 0.05), and from 293 +/- 66 nA to 206 +/- 44 nA (30% block, n = 5, P < 0.01), respectively, without affecting the current-voltage relationship. Prazosin 100 mumol.L-1 and yohimbine 100 mumol.L-1, which were specific blockers of alpha 1 and alpha 2 adrenoceptors respectively, did not show the inhibitory effect on ICa. Phentolamine 100 mumol.L-1 also inhibited the IK,ATP induced by 2, 4-dinitrophenol (DNP) at 0 mV from 3.2 +/- 0.6 nA to 0.8 +/- 0.5 nA (75% block, n = 4, P < 0.01). CONCLUSION: Phentolamine directly inhibits ICa and IK,ATP in guinea pig ventricular myocytes. (+info)Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (6/222)
Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters. (+info)Electrochemical and electrophysiological characterization of neurotransmitter release from sympathetic nerves supplying rat mesenteric arteries. (7/222)
1. Characteristic features of noradrenaline (NA) and adenosine 5'-triphosphate (ATP) release from postganglionic sympathetic nerves in rat small mesenteric arteries in vitro have been investigated on an impulse-by-impulse basis. NA release was measured using continuous amperometry and ATP release was monitored by intracellular recording of excitatory junction potentials (e.j.ps). 2. Electrical stimuli evoked transient increases in oxidation current. During trains of ten stimuli at 0.5 - 4 Hz there was a depression in the amplitude of oxidation currents evoked following the first stimulus in the train. 3. The neuronal NA uptake inhibitor, desmethylimipramine (1 microM), increased the amplitude of the summed oxidation current evoked by ten stimuli at 1 Hz and slowed the decay of oxidation currents evoked by trains of ten stimuli at 1 and 10 Hz. 4. The alpha2-adrenoceptor antagonist, idazoxan (1 microM), increased the amplitudes of the oxidation currents evoked during trains of ten stimuli at 0.5 - 10 Hz but had no effect on the oxidation currents evoked by the first stimulus in the train. 5. Idazoxan (1 microM) increased the amplitude of all e.j.ps evoked during trains of stimuli at 0.5 and 1 Hz. In addition, the facilitatory effect of idazoxan on e.j.ps was significantly greater than that on oxidation currents. 6. The findings indicate that NA release from sympathetic nerves supplying small mesenteric arteries is regulated by activation of presynaptic alpha2-adrenoceptors and that clearance of released NA in this tissue depends, in part, upon neuronal uptake. The different effects of idazoxan on the oxidation currents and e.j.ps may indicate that the release of NA and ATP is differentially modulated. (+info)Enhanced cortical dopamine output and antipsychotic-like effects of raclopride by alpha2 adrenoceptor blockade. (8/222)
Clozapine exerts superior clinical efficacy and markedly enhances cortical dopamine output compared with classical antipsychotic drugs. Here the alpha2 adrenoceptor antagonist idazoxan was administered to rats alone or in combination with the D2/3 dopamine receptor antagonist raclopride. Dopamine efflux in the medial prefrontal cortex and conditioned avoidance responding were analyzed. Idazoxan selectively potentiated the cortical output of dopamine and augmented the suppression of conditioned avoidance responding induced by raclopride. These results challenge basic assumptions underlying the dopamine hypothesis of schizophrenia and provide insight into clozapine's mode of action. (+info)Receptors, Adrenergic, alpha-2 are a type of protein found on the surface of cells in the body that bind to and respond to a class of hormones called catecholamines, including adrenaline and noradrenaline. These receptors are part of the body's autonomic nervous system and play a role in regulating a variety of physiological processes, including blood pressure, heart rate, and inflammation. Activation of alpha-2 receptors can cause a decrease in heart rate and blood pressure, as well as a decrease in inflammation and pain. They are found in many different tissues throughout the body, including the brain, heart, and blood vessels.
Interleukin 1 Receptor Antagonist Protein (IL-1Ra) is a protein that acts as an antagonist to the Interleukin 1 (IL-1) cytokine family. IL-1 is a group of signaling molecules that play a crucial role in the immune response and inflammation. IL-1Ra binds to the IL-1 receptor and prevents IL-1 from binding to its receptor, thereby inhibiting its pro-inflammatory effects. IL-1Ra is produced by various cells in the body, including monocytes, macrophages, and fibroblasts, and is released in response to inflammation or injury. It is also found in high concentrations in synovial fluid, which is the fluid that lubricates the joints. IL-1Ra has been shown to have anti-inflammatory and immunosuppressive effects, and it has been used in clinical trials to treat various inflammatory and autoimmune diseases, such as rheumatoid arthritis, psoriasis, and inflammatory bowel disease. It is also being studied as a potential treatment for COVID-19, as it may help to reduce inflammation and prevent severe illness.
Piperidines are a class of organic compounds that contain a six-membered ring with nitrogen atoms at positions 1 and 4. They are commonly used in the pharmaceutical industry as a building block for the synthesis of a wide range of drugs, including analgesics, anti-inflammatory agents, and antihistamines. Piperidines are also found in natural products, such as alkaloids, and have been used in traditional medicine for their various therapeutic effects. In the medical field, piperidines are often used as a starting point for the development of new drugs, as they can be easily modified to produce a wide range of pharmacological activities.
Angiotensin receptor antagonists (ARAs) are a class of medications used in the medical field to treat high blood pressure (hypertension) and heart failure. These drugs work by blocking the action of angiotensin II, a hormone that narrows blood vessels and increases blood pressure. By blocking this hormone, ARAs help to relax blood vessels and lower blood pressure, which can reduce the risk of heart attack, stroke, and other complications associated with hypertension and heart failure. ARAs are available in both oral and injectable forms and are often used in combination with other blood pressure-lowering medications.
Adenosine A2 receptor antagonists are a class of drugs that block the action of adenosine A2 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including blood flow, heart rate, and inflammation. The A2 receptors are a subfamily of adenosine receptors that are found in many different tissues throughout the body. Adenosine A2 receptor antagonists are used to treat a variety of conditions, including hypertension (high blood pressure), heart failure, and asthma. They work by blocking the action of adenosine on the A2 receptors, which can help to relax blood vessels and reduce blood pressure. In heart failure, A2 receptor antagonists can help to improve heart function and reduce the workload on the heart. In asthma, they can help to reduce inflammation and bronchoconstriction (narrowing of the airways). Some examples of adenosine A2 receptor antagonists include cilostazol, pirenzepine, and ZM-241385. These drugs are typically administered orally or intravenously, and their side effects can include headache, nausea, and dizziness. It is important to note that the use of adenosine A2 receptor antagonists should be closely monitored by a healthcare provider, as they can interact with other medications and may have potential side effects.
Hormone antagonists are medications that block or inhibit the effects of hormones in the body. They are often used in medical treatments to counteract the effects of hormones that are either overactive or underactive. Examples of hormone antagonists include: 1. Selective estrogen receptor modulators (SERMs): These medications block the effects of estrogen in some tissues but not others. They are used to treat conditions such as breast cancer and osteoporosis. 2. Progestins: These medications mimic the effects of the hormone progesterone and are used to treat conditions such as menopause symptoms and endometriosis. 3. Androgens: These medications block the effects of testosterone and are used to treat conditions such as prostate cancer and hirsutism (excessive hair growth in women). 4. Gonadotropin-releasing hormone (GnRH) antagonists: These medications block the release of gonadotropins, hormones that stimulate the ovaries and testes to produce sex hormones. They are used to treat conditions such as endometriosis and prostate cancer. Overall, hormone antagonists are an important tool in the medical field for treating a variety of conditions related to hormonal imbalances.
Adenosine A1 receptor antagonists are a class of drugs that block the action of adenosine A1 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including heart rate, blood pressure, and sleep. Adenosine A1 receptors are found in many different tissues throughout the body, including the brain, heart, and lungs. Adenosine A1 receptor antagonists are used to treat a variety of conditions, including Parkinson's disease, schizophrenia, and overactive bladder. They work by blocking the action of adenosine at A1 receptors, which can help to improve symptoms and reduce the risk of side effects associated with other treatments. Some examples of adenosine A1 receptor antagonists include caffeine, theophylline, and modafinil.
Receptors, Endothelin are a type of protein receptors found on the surface of cells in the endothelium, which is the inner lining of blood vessels. These receptors are activated by the hormone endothelin, which is produced by cells in the walls of blood vessels and plays a role in regulating blood pressure and blood vessel tone. Activation of endothelin receptors can cause blood vessels to constrict, which can increase blood pressure and reduce blood flow to organs and tissues. Endothelin receptors are also involved in the development of certain cardiovascular diseases, such as hypertension and heart failure.
Adrenergic alpha-1 receptor antagonists are a class of medications that block the action of alpha-1 adrenergic receptors in the body. These receptors are found in various tissues, including blood vessels, the heart, and the smooth muscle of the bronchial tubes. When activated by the hormone adrenaline (also known as epinephrine), alpha-1 receptors cause constriction of blood vessels, increased heart rate, and bronchoconstriction. Adrenergic alpha-1 receptor antagonists are used to treat a variety of conditions, including high blood pressure, heart disease, and certain types of anxiety disorders. They work by relaxing blood vessels, reducing blood pressure, and slowing the heart rate. They can also help to relieve symptoms of anxiety and panic attacks by reducing the physical symptoms of stress, such as rapid heart rate and sweating. Some examples of adrenergic alpha-1 receptor antagonists include prazosin (Minipress), doxazosin (Cardura), and terazosin (Hytrin). These medications are usually taken by mouth and are generally well-tolerated, although they can cause side effects such as dizziness, lightheadedness, and low blood pressure.
Sialoglycoproteins are a type of glycoprotein that are found in the saliva of humans and other animals. They are composed of a protein core and one or more carbohydrate chains attached to the protein. Sialoglycoproteins play important roles in a variety of biological processes, including the lubrication and protection of the oral mucosa, the breakdown of food in the mouth, and the immune response. They are also involved in the development and progression of certain diseases, such as cancer and autoimmune disorders. In the medical field, sialoglycoproteins are often studied as potential biomarkers for these and other conditions.
Receptors, Adrenergic, alpha (α-adrenergic receptors) are a type of protein found on the surface of cells in the body that bind to and respond to signaling molecules called catecholamines, such as adrenaline and noradrenaline. These receptors are involved in a wide range of physiological processes, including the regulation of blood pressure, heart rate, and metabolism. There are several different subtypes of α-adrenergic receptors, including α1A, α1B, and α1D receptors, which are found in different tissues throughout the body. Activation of these receptors can have a variety of effects, depending on the specific subtype and the tissue in which it is located. For example, activation of α1-adrenergic receptors in the heart can cause the heart to beat faster and stronger, while activation of α1-adrenergic receptors in the blood vessels can cause them to constrict, leading to an increase in blood pressure. α-adrenergic receptors are also involved in the body's response to stress and can be activated by the release of stress hormones such as cortisol. Activation of these receptors can help to prepare the body for the "fight or flight" response by increasing heart rate and blood pressure and redirecting blood flow to the muscles.
Alpha 1-Antitrypsin (AAT) is a protein produced by the liver that plays a crucial role in protecting the lungs from damage caused by enzymes called proteases. Proteases are enzymes that break down proteins, and in the lungs, they can cause inflammation and damage to the airways and lung tissue. AAT acts as a protease inhibitor, binding to and neutralizing proteases that would otherwise cause damage to the lungs. It is particularly important in protecting the lungs from damage caused by cigarette smoke, air pollution, and other irritants. Deficiency in AAT can lead to a condition called alpha 1-antitrypsin deficiency, which is a genetic disorder that can cause lung disease, liver disease, and other health problems. People with alpha 1-antitrypsin deficiency produce low levels of AAT or produce AAT that is not functional, leading to an increased risk of lung damage and other health problems.
Leukotriene antagonists are a class of medications that block the action of leukotrienes, which are chemical messengers produced by the immune system. These drugs are used to treat a variety of conditions, including asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis (hay fever). Leukotrienes play a role in the inflammatory response and can cause constriction of the airways, leading to difficulty breathing. By blocking the action of leukotrienes, leukotriene antagonists can help to relax the airways and improve breathing in people with asthma or COPD. There are several different types of leukotriene antagonists available, including montelukast (Singulair) and zafirlukast (Accolate). These drugs are usually taken by mouth and are generally well-tolerated. However, like all medications, they can cause side effects, such as headache, nausea, and dizziness. It is important to talk to a healthcare provider about the potential benefits and risks of leukotriene antagonists before starting treatment.
The Endothelin A receptor (ETA receptor) is a protein that is found on the surface of cells in the body, particularly in the endothelium (the inner lining of blood vessels). It is a type of G protein-coupled receptor, which means that it is activated by a molecule called an agonist, such as endothelin-1, and triggers a series of cellular responses. The ETA receptor plays a role in regulating blood pressure and blood vessel tone, and is also involved in the development and progression of certain diseases, such as hypertension, heart failure, and atherosclerosis. Activation of the ETA receptor can cause vasoconstriction (narrowing of blood vessels), which can increase blood pressure, and can also stimulate the release of other signaling molecules that can contribute to inflammation and tissue damage. In the medical field, the ETA receptor is an important target for the development of drugs that are used to treat cardiovascular diseases. For example, some drugs that block the ETA receptor, such as bosentan and ambrisentan, are used to treat pulmonary hypertension, a condition in which blood pressure in the lungs is abnormally high.
Receptors, Serotonin are proteins found on the surface of cells in the body that bind to serotonin, a neurotransmitter that plays a role in regulating mood, appetite, and other bodily functions. There are several different types of serotonin receptors, each of which has a specific function and is activated by different types of serotonin molecules. Dysfunction of serotonin receptors has been implicated in a number of mental health conditions, including depression, anxiety, and obsessive-compulsive disorder. Medications that target serotonin receptors, such as selective serotonin reuptake inhibitors (SSRIs), are commonly used to treat these conditions.
Receptors, N-Methyl-D-Aspartate (NMDA) are a type of ionotropic glutamate receptor found in the central nervous system. They are named after the agonist N-methyl-D-aspartate (NMDA), which binds to and activates these receptors. NMDA receptors are important for a variety of physiological processes, including learning and memory, synaptic plasticity, and neuroprotection. They are also involved in various neurological and psychiatric disorders, such as schizophrenia, depression, and addiction. NMDA receptors are heteromeric complexes composed of two subunits, NR1 and NR2, which can be differentially expressed in various brain regions and cell types. The NR2 subunit determines the pharmacological properties and functional profile of the receptor, while the NR1 subunit is essential for receptor function. Activation of NMDA receptors requires the binding of both glutamate and a co-agonist, such as glycine or d-serine, as well as the depolarization of the postsynaptic membrane. This leads to the opening of a cation-permeable channel that allows the influx of calcium ions, which can trigger various intracellular signaling pathways and modulate gene expression. In summary, NMDA receptors are a type of glutamate receptor that play a crucial role in various physiological and pathological processes in the central nervous system.
Dizocilpine maleate, also known as dizocilpine or dizocilpine dibromide, is a drug that belongs to a class of compounds called N-methyl-D-aspartate (NMDA) receptor antagonists. It is used in scientific research to study the effects of NMDA receptor antagonists on the brain and nervous system. In the medical field, dizocilpine maleate has been studied for its potential therapeutic effects in a variety of neurological and psychiatric conditions, including Parkinson's disease, Huntington's disease, and schizophrenia. However, it has not been approved for use in humans by regulatory agencies such as the US Food and Drug Administration (FDA) due to concerns about its safety and efficacy. Dizocilpine maleate is a potent and selective NMDA receptor antagonist that blocks the action of glutamate, a neurotransmitter that plays a key role in learning, memory, and other cognitive functions. It is believed that by blocking NMDA receptors, dizocilpine maleate can reduce the overactivity of neurons in the brain that is thought to contribute to the symptoms of certain neurological and psychiatric conditions. However, dizocilpine maleate has also been associated with a range of side effects, including cognitive impairment, psychosis, and motor dysfunction. As a result, its use in humans is limited and is typically only conducted in controlled clinical trials under the supervision of a qualified healthcare professional.
Receptors, Interleukin-1 (IL-1R) are a type of cell surface receptor that are activated by the cytokine interleukin-1 (IL-1). IL-1 is a signaling molecule that plays a key role in the immune response and inflammation. It is produced by immune cells in response to infection or injury and can stimulate the production of other cytokines, as well as activate immune cells such as macrophages and T cells. IL-1R are expressed on a variety of cell types, including immune cells, endothelial cells, and fibroblasts. When IL-1 binds to its receptor, it triggers a signaling cascade that leads to the activation of various intracellular signaling pathways, including the NF-ÎşB pathway and the MAPK pathway. These pathways can activate genes that produce pro-inflammatory molecules, such as cytokines and chemokines, as well as genes that regulate cell survival and proliferation. IL-1R are important in the regulation of the immune response and inflammation, and are also involved in the development of various diseases, including autoimmune diseases, inflammatory bowel disease, and cancer. Inhibitors of IL-1R or its downstream signaling pathways are being developed as potential therapeutic agents for these diseases.
Adrenergic alpha-2 receptor antagonists are a class of medications that block the action of adrenergic alpha-2 receptors in the body. These receptors are found in various tissues, including the heart, blood vessels, and central nervous system, and play a role in regulating blood pressure, heart rate, and other physiological processes. When adrenergic alpha-2 receptor antagonists are taken, they block the action of these receptors, leading to a variety of effects. For example, they can cause blood vessels to dilate, which can lower blood pressure, and they can increase heart rate and contractility, which can improve cardiac output. They can also have central nervous system effects, such as increasing alertness and reducing sedation. Adrenergic alpha-2 receptor antagonists are used to treat a variety of conditions, including hypertension, heart failure, and anxiety. They are also used in some cases of shock and as part of the treatment of certain types of cancer. Some examples of adrenergic alpha-2 receptor antagonists include clonidine, guanfacine, and moxonidine.
Adrenergic alpha-antagonists are a class of drugs that block the action of alpha-adrenergic receptors, which are a type of receptor found in the body that respond to the neurotransmitter norepinephrine (also known as noradrenaline). These receptors are found in various tissues throughout the body, including the blood vessels, heart, and bronchial muscles. When alpha-adrenergic receptors are activated by norepinephrine, they cause a variety of physiological responses, including constriction of blood vessels, increased heart rate and contractility, and bronchoconstriction. Adrenergic alpha-antagonists work by binding to these receptors and blocking their action, thereby reversing these effects. Adrenergic alpha-antagonists are used to treat a variety of conditions, including high blood pressure, heart disease, and glaucoma. They are also used to treat certain types of anxiety disorders and to prevent migraine headaches. Some examples of adrenergic alpha-antagonists include prazosin (Minipress), doxazosin (Cardura), and phentolamine (Regitine).
Biphenyl compounds are a class of organic compounds that consist of two benzene rings joined together by a single carbon-carbon bond. They are commonly used as industrial solvents, plasticizers, and flame retardants. In the medical field, biphenyl compounds have been studied for their potential therapeutic effects, including anti-inflammatory, anti-cancer, and anti-viral properties. Some biphenyl compounds have also been used as diagnostic agents in medical imaging. However, some biphenyl compounds have been associated with adverse health effects, including endocrine disruption, neurotoxicity, and carcinogenicity, and their use is regulated in many countries.
Benzazepines are a class of psychoactive drugs that are structurally related to benzodiazepines. They are characterized by the presence of a benzene ring fused to an azepine ring, which gives them their unique chemical structure and pharmacological properties. Benzazepines are primarily used as anxiolytics, sedatives, and hypnotics to treat conditions such as anxiety, insomnia, and agitation. They work by enhancing the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain, which helps to reduce anxiety and promote relaxation. Some examples of benzazepines include thienotriazolodiazepines (e.g., flunitrazepam), dibenzazepines (e.g., zolpidem), and benzodiazepine-like compounds (e.g., alprazolam). However, benzazepines are generally less commonly used than benzodiazepines due to their potential for abuse and dependence, as well as their side effects, which can include drowsiness, dizziness, and impaired coordination.
Tetrazoles are a class of organic compounds that contain a five-membered ring with four nitrogen atoms and one carbon atom. They have a variety of applications in the medical field, including as antimicrobial agents, anticancer drugs, and as inhibitors of enzymes involved in various biological processes. One example of a tetrazole-based drug is linezolid, which is an antibiotic used to treat bacterial infections, including pneumonia, skin infections, and bone and joint infections. Linezolid works by inhibiting the production of bacterial proteins, which are essential for the bacteria's survival. Tetrazoles are also being investigated as potential treatments for cancer. For example, some tetrazole derivatives have been shown to selectively target and kill cancer cells, while sparing healthy cells. Additionally, tetrazoles have been found to have anti-inflammatory and analgesic properties, which could make them useful in the treatment of pain and other inflammatory conditions. Overall, tetrazoles are a versatile class of compounds with a wide range of potential applications in the medical field.
Pyridines are a class of heterocyclic aromatic compounds that contain a six-membered ring with one nitrogen atom and five carbon atoms. They are commonly used in the medical field as precursors for the synthesis of various drugs and as ligands in metal complexes that have potential therapeutic applications. Some examples of drugs that contain pyridine rings include the antihistamine loratadine, the antipsychotic drug chlorpromazine, and the anti-inflammatory drug ibuprofen. Pyridines are also used as chelating agents to remove heavy metals from the body, and as corrosion inhibitors in the manufacturing of metal products.
Xanthines are a group of compounds that include caffeine, theophylline, and theobromine. They are naturally occurring alkaloids found in plants such as coffee, tea, and cocoa. In the medical field, xanthines are used as bronchodilators to treat conditions such as asthma and chronic obstructive pulmonary disease (COPD). They work by relaxing the muscles in the airways, allowing air to flow more easily. Xanthines can also be used to treat heart rhythm disorders and to prevent blood clots. However, they can have side effects such as nausea, vomiting, and increased heart rate, and may interact with other medications.
In the medical field, peptides are short chains of amino acids that are linked together by peptide bonds. Cyclic peptides are a type of peptide in which the amino acids are linked in a ring-like structure, rather than in a linear chain. These cyclic peptides can have a variety of biological activities, including antimicrobial, antiviral, and anti-inflammatory effects. They are being studied for their potential use in the development of new drugs and therapies.
Sulfonamides are a class of synthetic antimicrobial drugs that were first discovered in the 1930s. They are commonly used to treat a variety of bacterial infections, including urinary tract infections, respiratory infections, and skin infections. Sulfonamides work by inhibiting the production of folic acid by bacteria, which is essential for their growth and reproduction. They are often used in combination with other antibiotics to increase their effectiveness. Sulfonamides are generally well-tolerated, but can cause side effects such as nausea, vomiting, and allergic reactions in some people.
Indoles are a class of organic compounds that contain a six-membered aromatic ring with a nitrogen atom at one of the corners of the ring. They are commonly found in a variety of natural products, including some plants, bacteria, and fungi. In the medical field, indoles have been studied for their potential therapeutic effects, particularly in the treatment of cancer. Some indoles have been shown to have anti-inflammatory, anti-cancer, and anti-bacterial properties, and are being investigated as potential drugs for the treatment of various diseases.
In the medical field, "binding, competitive" refers to a type of interaction between a ligand (a molecule that binds to a receptor) and a receptor. Competitive binding occurs when two or more ligands can bind to the same receptor, but they do so in a way that limits the maximum amount of ligand that can bind to the receptor at any given time. In other words, when a ligand binds to a receptor, it competes with other ligands that may also be trying to bind to the same receptor. The binding of one ligand can prevent or reduce the binding of other ligands, depending on the relative affinities of the ligands for the receptor. Competitive binding is an important concept in pharmacology, as it helps to explain how drugs can interact with receptors in the body and how their effects can be influenced by other drugs or substances that may also be present. It is also important in the study of biological systems, where it can help to explain how molecules interact with each other in complex biological networks.
Pyrazoles are a class of heterocyclic compounds that contain a five-membered ring with one nitrogen atom and two carbon atoms. They are commonly used in the medical field as pharmaceuticals and as active ingredients in various drugs. Pyrazoles have a wide range of biological activities, including anti-inflammatory, antifungal, antiviral, and antihypertensive properties. Some examples of drugs that contain pyrazoles include: 1. Metformin: A medication used to treat type 2 diabetes. 2. Etoricoxib: A nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation. 3. Ritonavir: An antiretroviral drug used to treat HIV/AIDS. 4. Alendronate: A medication used to treat osteoporosis. 5. Cilostazol: A medication used to treat peripheral arterial disease. Pyrazoles are also used as research tools in the field of medicinal chemistry to develop new drugs with specific biological activities.
Hypoxia-inducible factor 1, alpha subunit (HIF-1α) is a protein that plays a critical role in the body's response to low oxygen levels (hypoxia). It is a transcription factor that regulates the expression of genes involved in oxygen transport, metabolism, and angiogenesis (the formation of new blood vessels). Under normal oxygen conditions, HIF-1α is rapidly degraded by the proteasome, a protein complex that breaks down unnecessary or damaged proteins. However, when oxygen levels drop, HIF-1α is stabilized and accumulates in the cell. This allows it to bind to specific DNA sequences and activate the transcription of genes involved in the body's response to hypoxia. HIF-1α is involved in a wide range of physiological processes, including erythropoiesis (the production of red blood cells), angiogenesis, and glucose metabolism. It is also implicated in the development of several diseases, including cancer, cardiovascular disease, and neurodegenerative disorders. In the medical field, HIF-1α is a target for drug development, as modulating its activity has the potential to treat a variety of conditions. For example, drugs that inhibit HIF-1α activity may be useful in treating cancer, as many tumors rely on HIF-1α to survive in low-oxygen environments. On the other hand, drugs that activate HIF-1α may be useful in treating conditions such as anemia or heart failure, where increased oxygen delivery is needed.
Quinoxalines are a class of heterocyclic compounds that contain two nitrogen atoms in a six-membered ring. They are often used as intermediates in the synthesis of other compounds, such as pharmaceuticals and agrochemicals. In the medical field, quinoxalines have been studied for their potential use as antiviral, antifungal, and antiparasitic agents. Some quinoxalines have also been shown to have anti-inflammatory and analgesic properties, and are being investigated as potential treatments for a variety of conditions, including cancer, Alzheimer's disease, and Parkinson's disease. However, more research is needed to fully understand the potential therapeutic applications of quinoxalines.
In the medical field, "Cells, Cultured" refers to cells that have been grown and maintained in a controlled environment outside of their natural biological context, typically in a laboratory setting. This process is known as cell culture and involves the isolation of cells from a tissue or organism, followed by their growth and proliferation in a nutrient-rich medium. Cultured cells can be derived from a variety of sources, including human or animal tissues, and can be used for a wide range of applications in medicine and research. For example, cultured cells can be used to study the behavior and function of specific cell types, to develop new drugs and therapies, and to test the safety and efficacy of medical products. Cultured cells can be grown in various types of containers, such as flasks or Petri dishes, and can be maintained at different temperatures and humidity levels to optimize their growth and survival. The medium used to culture cells typically contains a combination of nutrients, growth factors, and other substances that support cell growth and proliferation. Overall, the use of cultured cells has revolutionized medical research and has led to many important discoveries and advancements in the field of medicine.
Azepines are a class of organic compounds that contain a seven-membered ring with four nitrogen atoms and three carbon atoms. They are often used as a building block for the synthesis of other drugs and are also used as anticonvulsants, anxiolytics, and sedatives in the medical field. Some common examples of azepines include triazolam (a benzodiazepine used to treat anxiety and insomnia), alprazolam (another benzodiazepine used to treat anxiety and panic disorder), and meprobamate (an antianxiety medication).
Losartan is a medication used to treat high blood pressure (hypertension) and to reduce the risk of stroke in people with high blood pressure and diabetes. It belongs to a class of drugs called angiotensin II receptor blockers (ARBs), which work by relaxing blood vessels and decreasing the workload on the heart. Losartan is also used to treat heart failure and to reduce the risk of heart attack in people who have had a heart attack or who have certain risk factors for heart disease. It is usually taken once or twice a day, with or without food. Common side effects of losartan include headache, dizziness, and cough.
Endothelin-1 (ET-1) is a potent vasoconstrictor peptide hormone that is primarily produced by endothelial cells in the walls of blood vessels. It plays a key role in regulating blood pressure and blood vessel tone, and is also involved in a variety of other physiological processes, including cell growth and differentiation, inflammation, and angiogenesis (the formation of new blood vessels). In the medical field, ET-1 is often measured as a biomarker for various cardiovascular diseases, such as hypertension, heart failure, and atherosclerosis. It is also used as a therapeutic target in the treatment of these conditions, with drugs such as endothelin receptor antagonists (ERAs) being developed to block the effects of ET-1 and improve cardiovascular outcomes. Additionally, ET-1 has been implicated in the pathogenesis of other diseases, such as cancer and fibrosis, and is being studied as a potential therapeutic target in these conditions as well.
Substance P is a neuropeptide that is involved in the transmission of pain signals in the nervous system. It is a small protein that is produced by sensory neurons in the peripheral nervous system and is released into the spinal cord and brain when these neurons are activated by noxious stimuli such as injury or inflammation. Substance P acts on specific receptors on nerve cells in the spinal cord and brain, triggering the release of other neurotransmitters and hormones that contribute to the perception of pain. It is also involved in other physiological processes, such as regulating blood pressure and heart rate. In the medical field, substance P is often studied in the context of pain management and the development of new pain medications. It is also used as a diagnostic tool in certain conditions, such as inflammatory bowel disease and irritable bowel syndrome, where it may be present in higher levels in the body.
The alpha7 nicotinic acetylcholine receptor (α7nAChR) is a type of ion channel protein found on the surface of certain cells in the nervous system. It is activated by the neurotransmitter acetylcholine, which is released by nerve cells (neurons) to communicate with each other. The α7nAChR plays a role in a number of important functions in the brain and body, including learning and memory, mood regulation, and muscle movement. It is also involved in the development and progression of certain neurological disorders, such as Alzheimer's disease, Parkinson's disease, and schizophrenia. In the medical field, the α7nAChR is being studied as a potential target for the development of new treatments for these and other conditions. For example, drugs that selectively activate the α7nAChR are being investigated as potential treatments for cognitive decline and other symptoms associated with Alzheimer's disease.
Serotonin is a neurotransmitter, a chemical messenger that transmits signals between nerve cells in the brain and throughout the body. It plays a crucial role in regulating mood, appetite, sleep, and other bodily functions. In the medical field, serotonin is often studied in relation to mental health conditions such as depression, anxiety, and obsessive-compulsive disorder (OCD). Low levels of serotonin have been linked to these conditions, and medications such as selective serotonin reuptake inhibitors (SSRIs) are often prescribed to increase serotonin levels in the brain and improve symptoms. Serotonin is also involved in the regulation of pain perception, blood pressure, and other bodily functions. Imbalances in serotonin levels have been implicated in a variety of medical conditions, including migraines, fibromyalgia, and irritable bowel syndrome (IBS).
Receptors, Bradykinin are a type of protein receptors found on the surface of cells in the body that bind to and respond to the hormone bradykinin. Bradykinin is a peptide hormone that plays a role in the inflammatory response and is involved in the regulation of blood pressure, pain, and other physiological processes. When bradykinin binds to its receptors, it triggers a cascade of chemical reactions within the cell that leads to various physiological effects. There are two main types of bradykinin receptors: B1 receptors and B2 receptors. B1 receptors are primarily found in the immune system and are involved in the inflammatory response, while B2 receptors are found in a wide range of tissues and are involved in a variety of physiological processes, including blood pressure regulation and pain perception.
Cimetidine is a medication that is primarily used to treat ulcers in the stomach and esophagus. It works by blocking the production of stomach acid, which can help to reduce pain and inflammation associated with ulcers. Cimetidine is also sometimes used to treat other conditions, such as heartburn, GERD (gastroesophageal reflux disease), and certain types of cancer. It is available in both oral and intravenous forms, and is typically taken two to four times per day. Side effects of cimetidine may include headache, dizziness, nausea, and constipation. It is important to follow the dosage instructions provided by your healthcare provider and to let them know if you experience any side effects while taking this medication.
Receptors, Neurokinin-1 (NK1 receptors) are a type of G protein-coupled receptor found on the surface of certain cells in the body, including nerve cells (neurons) and immune cells. These receptors are activated by a group of signaling molecules called neurokinins, which are released by nerve cells in response to various stimuli, such as injury, stress, or inflammation. NK1 receptors play a role in a number of physiological processes, including pain perception, inflammation, and regulation of the immune system. They are also involved in the development of certain diseases, such as chronic pain, asthma, and irritable bowel syndrome. In the medical field, NK1 receptors are targeted by drugs used to treat a variety of conditions, including pain, nausea, and inflammation. One example of a drug that targets NK1 receptors is aprepitant, which is used to prevent nausea and vomiting caused by chemotherapy. Other drugs that target NK1 receptors include telaprevir and maraviroc, which are used to treat hepatitis C and HIV, respectively.
Adenosine A3 receptor antagonists are a class of drugs that block the action of adenosine A3 receptors, which are a type of cell receptor found in various tissues throughout the body. These receptors play a role in regulating a number of physiological processes, including inflammation, pain, and cardiovascular function. Adenosine A3 receptor antagonists are being studied for their potential therapeutic applications in a variety of conditions, including chronic obstructive pulmonary disease (COPD), asthma, and cardiovascular disease. They may also have potential as treatments for certain types of cancer and neurological disorders. Some examples of adenosine A3 receptor antagonists that have been studied in clinical trials include MRS1191, MRS1522, and MRS1754. These drugs are typically administered orally or intravenously, and their side effects and potential interactions with other medications will depend on the specific drug being used.
The Endothelin B receptor (ETB) is a protein that is found on the surface of cells in the body, including cells in the cardiovascular system. It is a type of G protein-coupled receptor, which means that it is activated by the binding of a signaling molecule called an agonist, such as endothelin-1 or endothelin-3. When the ETB receptor is activated, it triggers a series of intracellular signaling events that can have a variety of effects on the cell, depending on the specific cell type and the context in which the receptor is activated. In the cardiovascular system, the ETB receptor is thought to play a role in regulating blood pressure and blood vessel tone, and it has been implicated in a number of cardiovascular diseases, including hypertension, heart failure, and atherosclerosis.
Piperazines are a class of organic compounds that contain a six-membered ring with two nitrogen atoms. They are commonly used in the medical field as drugs and are known for their anticholinergic, antispasmodic, and sedative properties. Some examples of piperazine-based drugs include antihistamines, antipsychotics, and antidiarrheals. Piperazines can also be used as intermediates in the synthesis of other drugs.
In the medical field, "Behavior, Animal" refers to the study of the actions, responses, and interactions of animals, including humans, with their environment. This field encompasses a wide range of topics, including animal behavior in the wild, animal behavior in captivity, animal behavior in domestic settings, and animal behavior in laboratory settings. Animal behaviorists study a variety of behaviors, including social behavior, mating behavior, feeding behavior, communication behavior, and aggression. They use a variety of research methods, including observational studies, experiments, and surveys, to understand the underlying mechanisms that drive animal behavior. Animal behavior research has important applications in fields such as conservation biology, animal welfare, and veterinary medicine. For example, understanding animal behavior can help conservationists develop effective strategies for protecting endangered species, and it can help veterinarians develop more effective treatments for behavioral disorders in animals.
Pyrrolidines are a class of organic compounds that contain a five-membered ring with four carbon atoms and one nitrogen atom. They are commonly used in the medical field as pharmaceuticals, as well as in the synthesis of other drugs and chemicals. One example of a pyrrolidine used in medicine is metoclopramide, which is used to treat nausea and vomiting. Another example is pyrilamine, which is used to treat allergies and hay fever. Pyrrolidines can also be used as chiral auxiliaries in organic synthesis, which allows for the synthesis of enantiomerically pure compounds. This is important in the pharmaceutical industry, as many drugs are effective only when administered in a specific enantiomer. Overall, pyrrolidines are a versatile class of compounds with a wide range of applications in the medical field.
Receptors, Adrenergic, alpha-1 are a type of protein receptors found on the surface of cells in the body that bind to and respond to certain hormones and neurotransmitters, specifically norepinephrine and epinephrine. These receptors are classified as alpha-1 receptors because they are activated by alpha-1 adrenergic agonists, which are drugs that mimic the effects of norepinephrine and epinephrine. Alpha-1 receptors are found in many different tissues throughout the body, including the heart, blood vessels, lungs, and urinary bladder. They play a role in a variety of physiological processes, including regulating blood pressure, heart rate, and smooth muscle contraction. When norepinephrine or epinephrine binds to an alpha-1 receptor, it triggers a series of chemical reactions within the cell that ultimately lead to the activation of various signaling pathways. These pathways can have a variety of effects, depending on the specific type of alpha-1 receptor and the tissue in which it is located. Alpha-1 receptors are also targeted by certain drugs, such as alpha-1 adrenergic blockers, which are used to treat conditions such as high blood pressure, benign prostatic hyperplasia, and urinary incontinence. These drugs work by blocking the binding of norepinephrine and epinephrine to alpha-1 receptors, thereby reducing their effects on the body.
Interleukin-1 (IL-1) is a type of cytokine, which is a signaling molecule that plays a crucial role in the immune system. IL-1 is produced by various types of immune cells, including macrophages, monocytes, and dendritic cells, in response to infection, injury, or inflammation. IL-1 has multiple functions in the immune system, including promoting the activation and proliferation of immune cells, enhancing the production of other cytokines, and regulating the inflammatory response. It can also stimulate the production of fever, which helps to fight off infections. In the medical field, IL-1 is often studied in the context of various diseases, including autoimmune disorders, inflammatory bowel disease, and rheumatoid arthritis. It is also being investigated as a potential target for the development of new treatments for these conditions.
Receptors, Cholecystokinin (CCK) are a type of protein receptor found in the cells of various organs in the body, including the pancreas, small intestine, and brain. These receptors are activated by the hormone cholecystokinin, which is produced by the cells of the small intestine in response to the presence of food in the stomach. When cholecystokinin binds to its receptors, it triggers a series of chemical reactions that lead to the release of digestive enzymes from the pancreas and the contraction of the muscles of the small intestine. This helps to move food through the digestive system and prepare it for absorption. In addition to its role in digestion, cholecystokinin has been found to play a role in regulating appetite, mood, and other physiological processes. It is also involved in the development of certain types of cancer, including pancreatic cancer. Overall, receptors, cholecystokinin are an important part of the body's digestive system and play a role in regulating a variety of physiological processes.
Devazepide is a medication used to treat high blood pressure (hypertension) and to reduce the risk of stroke and heart attack in people with high blood pressure and diabetes. It belongs to a class of drugs called diuretics, which work by increasing the amount of urine produced by the kidneys, which helps to lower blood pressure. Devazepide is taken by mouth and is usually prescribed once or twice a day. It is important to follow the instructions of your healthcare provider and to take the medication as directed. Devazepide may cause side effects, such as dizziness, headache, and stomach upset. It is important to talk to your healthcare provider if you experience any side effects while taking this medication.
Adrenergic antagonists are a class of drugs that block the action of adrenalin or noradrenaline, which are hormones that stimulate the sympathetic nervous system. These drugs are used to treat a variety of conditions, including high blood pressure, heart disease, and anxiety disorders. They work by blocking the receptors on cells that respond to adrenalin and noradrenaline, preventing these hormones from triggering a response. There are several different types of adrenergic antagonists, including beta blockers, alpha blockers, and mixed alpha and beta blockers. Beta blockers are used to treat high blood pressure, heart disease, and certain types of tremors, while alpha blockers are used to treat conditions such as high blood pressure, benign prostatic hyperplasia, and urinary incontinence. Mixed alpha and beta blockers are used to treat conditions such as hypertension and angina.
Prazosin is a medication that is used to treat high blood pressure (hypertension) and certain heart conditions, such as angina (chest pain) and heart failure. It belongs to a class of drugs called alpha blockers, which work by relaxing blood vessels and decreasing the workload on the heart. Prazosin is usually taken by mouth, and the dosage and duration of treatment will depend on the specific condition being treated and the individual patient's response to the medication. Common side effects of prazosin include dizziness, lightheadedness, and low blood pressure. It is important to follow the instructions of a healthcare provider when taking prazosin and to report any side effects that occur.
Receptors, Thromboxane are a type of protein receptors found on the surface of cells in the body that bind to and respond to thromboxane, a hormone-like substance that plays a role in blood clotting and inflammation. These receptors are involved in a variety of physiological processes, including platelet aggregation, vasoconstriction, and smooth muscle contraction. In the medical field, the study of thromboxane receptors is important for understanding the pathophysiology of various diseases, including cardiovascular disease, asthma, and inflammatory disorders.
Receptors, Vasopressin are proteins found on the surface of cells in the body that bind to and respond to the hormone vasopressin. Vasopressin is produced by the hypothalamus and released by the posterior pituitary gland. It plays a role in regulating water balance in the body by constricting blood vessels and increasing the reabsorption of water in the kidneys. Vasopressin receptors are also found in other parts of the body, including the brain, heart, and blood vessels, where they can have a variety of effects, including regulating blood pressure and promoting the growth of blood vessels.
Ketanserin is a medication that belongs to a class of drugs called serotonin receptor antagonists. It is primarily used to treat high blood pressure and Raynaud's phenomenon, a condition characterized by cold, white fingers and toes. Ketanserin works by blocking the action of serotonin, a neurotransmitter that plays a role in regulating blood pressure and blood vessel constriction. It is available in both oral and intravenous forms.
2-Amino-5-phosphonovalerate (APV) is a chemical compound that is used in the medical field as a drug. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, which means that it blocks the action of NMDA receptors in the brain. NMDA receptors are a type of ion channel that are involved in a variety of brain functions, including learning, memory, and mood regulation. By blocking NMDA receptors, APV can have a range of effects on the brain, including reducing seizures, improving mood, and reducing anxiety. APV is sometimes used as a treatment for conditions such as epilepsy, depression, and anxiety disorders. It is also being studied as a potential treatment for other neurological and psychiatric conditions.
In the medical field, "Disease Models, Animal" refers to the use of animals to study and understand human diseases. These models are created by introducing a disease or condition into an animal, either naturally or through experimental manipulation, in order to study its progression, symptoms, and potential treatments. Animal models are used in medical research because they allow scientists to study diseases in a controlled environment and to test potential treatments before they are tested in humans. They can also provide insights into the underlying mechanisms of a disease and help to identify new therapeutic targets. There are many different types of animal models used in medical research, including mice, rats, rabbits, dogs, and monkeys. Each type of animal has its own advantages and disadvantages, and the choice of model depends on the specific disease being studied and the research question being addressed.
The term "Receptor, Cannabinoid, CB1" refers to a specific type of protein found on the surface of certain cells in the human body. These proteins, called CB1 receptors, are activated by a class of chemicals called cannabinoids, which are found in the plant Cannabis sativa (marijuana) and in the body itself. CB1 receptors are primarily located in the brain and central nervous system, but they are also found in other parts of the body, such as the immune system, the gastrointestinal tract, and the reproductive system. When activated by cannabinoids, CB1 receptors can affect a wide range of physiological processes, including mood, pain perception, appetite, memory, and movement. In the medical field, CB1 receptors have been the subject of extensive research due to their potential therapeutic applications. For example, some studies have suggested that drugs that block CB1 receptors may be effective in treating conditions such as obesity, anxiety, and depression. On the other hand, drugs that activate CB1 receptors may be useful in treating conditions such as chronic pain, nausea, and muscle spasms. However, the use of cannabis and cannabinoid-based medications is still a controversial issue, and more research is needed to fully understand their potential benefits and risks.
Benzimidazoles are a class of organic compounds that contain a six-membered ring with two nitrogen atoms and two carbon atoms. They are widely used in the medical field as drugs and as active ingredients in pesticides. In the medical field, benzimidazoles are used to treat a variety of conditions, including: 1. Helminth infections: Benzimidazoles are effective against a range of parasitic worms, including roundworms, tapeworms, and flukes. They work by interfering with the worms' ability to absorb glucose, which leads to their death. 2. Gastric ulcers: Benzimidazoles are used to treat stomach ulcers caused by the bacteria Helicobacter pylori. They work by inhibiting the production of enzymes that break down the stomach lining, allowing the ulcers to heal. 3. Migraines: Benzimidazoles are sometimes used to prevent migraines by reducing inflammation in the brain. 4. Cancers: Some benzimidazoles are being studied as potential treatments for certain types of cancer, including colon cancer and ovarian cancer. Overall, benzimidazoles are a versatile class of compounds with a wide range of potential medical applications.
Receptors, Dopamine D2 are a type of protein found on the surface of cells in the brain and other parts of the body. These receptors are activated by the neurotransmitter dopamine, which is a chemical that helps to regulate a variety of functions in the brain, including movement, motivation, and reward. When dopamine binds to D2 receptors, it can cause a variety of effects, including reducing the activity of certain neurons and increasing the activity of others. This can lead to changes in behavior, mood, and other physiological processes. D2 receptors are also involved in the treatment of certain medical conditions, such as Parkinson's disease and schizophrenia, and are the target of many medications used to treat these conditions.
Adenosine is a naturally occurring nucleoside that plays a crucial role in various physiological processes in the human body. It is a component of the nucleic acids DNA and RNA and is also found in high concentrations in the cells of the heart, brain, and other organs. In the medical field, adenosine is often used as a medication to treat certain heart conditions, such as supraventricular tachycardia (SVT) and atrial fibrillation (AFib). Adenosine works by blocking the electrical signals that cause the heart to beat too fast or irregularly. It is typically administered as an intravenous injection and has a short duration of action, lasting only a few minutes. Adenosine is also used in research to study the function of various cells and tissues in the body, including the nervous system, immune system, and cardiovascular system. It has been shown to have a wide range of effects on cellular signaling pathways, including the regulation of gene expression, cell proliferation, and apoptosis (cell death).
Naltrexone is a medication that is used to treat alcohol and opioid addiction. It works by blocking the effects of opioids and alcohol on the brain, which can help reduce cravings and prevent relapse. Naltrexone is available in both oral and injectable forms, and it is typically prescribed as part of a comprehensive treatment plan that may also include counseling and support. It is important to note that naltrexone is not effective for everyone, and it may not be suitable for people with certain medical conditions or who are taking certain medications. It is always important to discuss the potential risks and benefits of any medication with a healthcare provider before starting treatment.
Adrenergic alpha-agonists are drugs that bind to and activate alpha-adrenergic receptors, which are a type of G protein-coupled receptor found in various tissues throughout the body. These receptors are involved in a wide range of physiological processes, including the regulation of blood pressure, heart rate, and smooth muscle contraction. When an adrenergic alpha-agonist binds to an alpha-adrenergic receptor, it causes the receptor to activate a signaling cascade that ultimately leads to the production of cyclic AMP (cAMP). This increase in cAMP can cause a variety of effects, depending on the specific tissue and receptor subtype involved. For example, in the heart, alpha-adrenergic receptor activation can increase heart rate and contractility, while in the blood vessels, it can cause vasoconstriction (narrowing of the blood vessels). Adrenergic alpha-agonists are used in a variety of medical settings, including the treatment of hypertension, heart failure, and bronchospasm (narrowing of the airways in the lungs). They are also used as part of anesthesia to help control blood pressure and heart rate during surgery. Some examples of adrenergic alpha-agonists include epinephrine, norepinephrine, and phenylephrine.
Famotidine is a medication that is used to treat conditions such as heartburn, acid reflux, and stomach ulcers. It works by blocking the production of stomach acid, which helps to reduce symptoms such as heartburn and acid reflux. Famotidine is available in both over-the-counter and prescription forms, and is typically taken by mouth. It is generally considered to be safe and effective when used as directed, but like all medications, it can cause side effects in some people. Some common side effects of famotidine include headache, dizziness, and nausea.
Receptors, Neurokinin-2 (NK2) are a type of G protein-coupled receptor found in the nervous system. They are activated by the neuropeptide substance P, which is involved in pain transmission and regulation of the immune system. Activation of NK2 receptors can lead to a variety of physiological responses, including vasodilation, increased heart rate, and bronchoconstriction. These receptors are also involved in the regulation of mood and anxiety, and have been implicated in the pathophysiology of certain neurological disorders, such as depression and schizophrenia.
Calcium is a chemical element with the symbol Ca and atomic number 20. It is a vital mineral for the human body and is essential for many bodily functions, including bone health, muscle function, nerve transmission, and blood clotting. In the medical field, calcium is often used to diagnose and treat conditions related to calcium deficiency or excess. For example, low levels of calcium in the blood (hypocalcemia) can cause muscle cramps, numbness, and tingling, while high levels (hypercalcemia) can lead to kidney stones, bone loss, and other complications. Calcium supplements are often prescribed to people who are at risk of developing calcium deficiency, such as older adults, vegetarians, and people with certain medical conditions. However, it is important to note that excessive calcium intake can also be harmful, and it is important to follow recommended dosages and consult with a healthcare provider before taking any supplements.
Bradykinin is a peptide hormone that plays a role in the regulation of blood pressure, inflammation, and pain. It is produced in the body by the breakdown of larger proteins called kinins, which are released from blood vessels and other tissues in response to injury or inflammation. Bradykinin acts on various types of cells in the body, including blood vessels, smooth muscle cells, and nerve cells, to cause a range of physiological effects. In the blood vessels, bradykinin causes them to dilate, or widen, which can lead to a drop in blood pressure. It also increases the permeability of blood vessels, allowing fluid and other substances to leak out and cause swelling. In addition to its effects on blood vessels, bradykinin is also involved in the body's inflammatory response. It stimulates the release of other inflammatory mediators, such as prostaglandins and leukotrienes, which can cause redness, swelling, and pain. Overall, bradykinin plays an important role in the body's response to injury and inflammation, and its activity is tightly regulated by various enzymes and other factors in the body.
Cannabinoid Receptor Antagonists are a class of drugs that block the effects of cannabinoids, which are naturally occurring chemicals found in the cannabis plant. These drugs work by binding to the same receptors in the brain as cannabinoids, but they prevent the cannabinoids from activating these receptors and producing their effects. Cannabinoid receptor antagonists are used in the medical field to treat a variety of conditions, including anxiety, depression, and addiction. They are also being studied for their potential use in treating other conditions, such as chronic pain, multiple sclerosis, and epilepsy. Some examples of cannabinoid receptor antagonists include rimonabant (which was withdrawn from the market due to safety concerns), nabilone, and dronabinol. These drugs are typically administered orally and can produce side effects such as nausea, insomnia, and anxiety.
Naloxone is a medication used to reverse the effects of opioid overdose. It works by binding to opioid receptors in the brain and body, blocking the effects of opioids and causing the person to breathe normally again. Naloxone is often administered as an injection, but it can also be administered nasally or intravenously. It is commonly used in emergency medical settings to treat opioid overdose, but it can also be used in non-emergency situations, such as in the management of chronic pain or opioid addiction.
Quinuclidines are a class of organic compounds that contain a quinuclidine ring, which is a six-membered ring with four nitrogen atoms and two carbon atoms. They are structurally related to the amphetamines and have been used as stimulants and nootropics. Some quinuclidines, such as pyrovalerone, have also been used as analgesics and anticonvulsants. In the medical field, quinuclidines are not commonly used and their therapeutic potential is not well established.
Benzodiazepinones are a class of psychoactive drugs that are similar in structure to benzodiazepines, but with some key differences. Like benzodiazepines, benzodiazepinones are used to treat a variety of conditions, including anxiety, insomnia, and muscle spasms. However, benzodiazepinones are generally considered to be less potent and have a shorter duration of action than benzodiazepines. Benzodiazepinones are classified as Schedule IV controlled substances in the United States, meaning that they have a low potential for abuse and dependence. However, like all psychoactive drugs, benzodiazepinones can be habit-forming and should be used only under the guidance of a healthcare professional.
Histamine is a chemical substance that is produced by certain cells in the body, including immune cells and cells in the digestive system. It plays a role in a variety of physiological processes, including the contraction of smooth muscles, the dilation of blood vessels, and the stimulation of nerve endings. In the medical field, histamine is often used as a diagnostic tool to help identify conditions such as allergies, asthma, and certain types of infections. It is also used as a treatment for certain conditions, such as allergic reactions and certain types of digestive disorders.
Adrenergic beta-2 receptor antagonists, also known as beta blockers, are a class of medications that block the action of adrenaline (epinephrine) and noradrenaline (norepinephrine) on the beta-2 receptors in the body. These receptors are found in various organs and tissues, including the heart, lungs, and blood vessels. When adrenaline and noradrenaline bind to beta-2 receptors, they cause a number of physiological responses, such as increased heart rate, blood pressure, and bronchodilation (dilation of the airways in the lungs). Beta blockers work by blocking these receptors, thereby reducing the effects of adrenaline and noradrenaline on the body. Beta blockers are commonly used to treat a variety of conditions, including high blood pressure, heart disease, and certain types of tremors. They can also be used to treat anxiety and panic disorders, as well as to prevent migraines. However, they are not suitable for everyone and should only be taken under the guidance of a healthcare professional.
Bicuculline is a chemical compound that is commonly used in the medical field as a muscle relaxant and as a tool for studying the function of the central nervous system. It is a non-competitive antagonist of the gamma-aminobutyric acid (GABA) receptor, which is a type of ion channel that is involved in the regulation of muscle tone and other functions in the brain and spinal cord. Bicuculline is typically administered intravenously or intramuscularly, and it can cause a range of effects, including muscle relaxation, sedation, and changes in heart rate and blood pressure. It is also used in research to study the role of GABA receptors in various neurological disorders, such as epilepsy and anxiety disorders. It is important to note that bicuculline can be toxic in high doses and can cause serious side effects, including respiratory depression, seizures, and coma. As such, it is typically only used under the supervision of a qualified healthcare professional.
Receptors, Nicotinic are a type of neurotransmitter receptor found in the nervous system that are activated by the neurotransmitter acetylcholine. These receptors are involved in a variety of physiological processes, including muscle contraction, heart rate regulation, and the regulation of breathing. They are also found in the brain and are thought to play a role in learning, memory, and mood regulation. In the medical field, the study of nicotinic receptors is important for understanding the effects of nicotine, which is the primary psychoactive substance in tobacco, as well as for the development of drugs for the treatment of conditions such as Alzheimer's disease and schizophrenia.
Imidazoles are a class of organic compounds that contain a five-membered heterocyclic ring with two nitrogen atoms and three carbon atoms. In the medical field, imidazoles are commonly used as antifungal agents, particularly for the treatment of dermatophytic infections such as athlete's foot, ringworm, and jock itch. They work by inhibiting the growth of fungi by interfering with their metabolism. One of the most well-known imidazole antifungal agents is clotrimazole, which is used topically to treat skin and nail infections caused by fungi. Other imidazole antifungal agents include miconazole, ketoconazole, and itraconazole, which are used to treat a variety of fungal infections, including systemic infections such as cryptococcal meningitis and aspergillosis. Imidazoles are also used in other medical applications, such as in the treatment of parasitic infections, as well as in the development of new drugs for the treatment of cancer and other diseases.
Interleukin-1alpha (IL-1α) is a type of cytokine, which is a signaling molecule that plays a crucial role in the immune system. It is produced by a variety of cells, including macrophages, monocytes, and dendritic cells, in response to infection, injury, or inflammation. IL-1α is involved in the regulation of immune responses, including the activation of T cells, B cells, and natural killer cells. It also plays a role in the production of other cytokines and chemokines, which help to recruit immune cells to the site of infection or injury. In addition to its role in the immune system, IL-1α has been implicated in a number of other physiological processes, including the regulation of bone metabolism, the control of blood pressure, and the regulation of pain perception. Abnormal levels of IL-1α have been associated with a number of medical conditions, including inflammatory diseases such as rheumatoid arthritis and psoriasis, as well as neurodegenerative diseases such as Alzheimer's and Parkinson's. As such, IL-1α is an important target for the development of new therapeutic strategies for these conditions.
Mineralocorticoid receptor antagonists (MRAs) are a class of medications that block the action of aldosterone, a hormone produced by the adrenal gland that regulates the balance of salt and water in the body. Aldosterone acts on mineralocorticoid receptors in various tissues, including the kidney, heart, and blood vessels, to increase sodium reabsorption, reduce potassium excretion, and constrict blood vessels. MRAs are primarily used to treat hypertension (high blood pressure) by reducing sodium reabsorption in the kidneys and relaxing blood vessels. They are also used to treat heart failure, as they can reduce the workload on the heart by reducing blood volume and improving blood flow to the heart muscle. Additionally, MRAs are used to treat certain types of kidney disease, such as primary aldosteronism, by reducing the production of aldosterone. Examples of MRAs include spironolactone, eplerenone, and canrenone. These medications are typically taken orally and may be used alone or in combination with other antihypertensive medications. It is important to note that MRAs can cause side effects, such as potassium depletion, fluid retention, and gynecomastia (enlargement of the breasts in men), and should be used under the guidance of a healthcare provider.
Receptors, Histamine H3 are a type of protein found on the surface of cells in the body that bind to the neurotransmitter histamine. These receptors are classified as G protein-coupled receptors (GPCRs) and are activated by histamine, which is a chemical messenger that is involved in a variety of physiological processes, including allergic reactions, sleep regulation, and the regulation of appetite and body weight. There are two main types of histamine receptors: H1 receptors and H2 receptors. H1 receptors are found on cells in the immune system, the central nervous system, and other tissues throughout the body. They are involved in the mediation of allergic reactions and the regulation of sleep. H2 receptors are found on cells in the stomach and other organs and are involved in the regulation of gastric acid secretion. H3 receptors are a relatively recently discovered type of histamine receptor. They are found on cells in the brain and other tissues throughout the body and are thought to play a role in the regulation of various physiological processes, including sleep, appetite, and body weight. However, the exact function of H3 receptors is not yet fully understood, and more research is needed to fully understand their role in the body.
Blood pressure is the force exerted by the blood against the walls of the blood vessels as the heart pumps blood through the body. It is measured in millimeters of mercury (mmHg) and is typically expressed as two numbers: systolic pressure (the pressure when the heart beats) and diastolic pressure (the pressure when the heart is at rest between beats). Normal blood pressure is considered to be below 120/80 mmHg, while high blood pressure (hypertension) is defined as a systolic pressure of 140 mmHg or higher and/or a diastolic pressure of 90 mmHg or higher. High blood pressure is a major risk factor for heart disease, stroke, and other health problems.
Yohimbine is a chemical compound that is derived from the bark of the yohimbe tree (Pausinystalia johimbe). It has been used in traditional medicine for centuries to treat various conditions, including erectile dysfunction, depression, and weight loss. In the medical field, yohimbine is primarily used as a medication to treat erectile dysfunction. It works by blocking the action of an enzyme called alpha-2 adrenergic receptors, which can cause blood vessels to constrict and reduce blood flow to the penis. By blocking these receptors, yohimbine can help to increase blood flow to the penis and improve erectile function. Yohimbine is available as a prescription medication and is typically taken orally. It can cause side effects, including headache, nausea, dizziness, and increased heart rate. It is important to note that yohimbine can interact with other medications, including antidepressants and blood pressure medications, so it should only be taken under the supervision of a healthcare provider.
Receptors, Opioid are specialized proteins found on the surface of cells in the body that bind to opioid drugs, such as morphine, heroin, and oxycodone. These receptors are part of the body's natural pain-relieving system and are involved in regulating pain, mood, and reward. When opioid drugs bind to these receptors, they can produce a range of effects, including pain relief, sedation, and euphoria. However, long-term use of opioid drugs can lead to dependence and addiction, as the body becomes accustomed to the presence of the drug and requires more of it to achieve the same effect.
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Agonists9
- These agents compete with beta-adrenergic agonists for available beta-receptor sites. (medscape.com)
- It has been widely established that dopamine and its agonists play an important role in cardiovascular, renal, hormonal, and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. (biopsychiatry.com)
- From a therapeutic point of view, the above-mentioned agonists are used for treating Parkinson's disease, acting over DA 2 dopaminergic receptors of the nigrostriatal system. (biopsychiatry.com)
- Bromocriptine and the other dopaminergic agonists mentioned act over DA 2 receptors of the tuberoinfundibular system, inhibiting prolactin release and decreasing hyperprolactinemia and tumor size. (biopsychiatry.com)
- This chapter discusses two groups of drugs that affect the sympathetic nervous system-adrenergic agonists, or sympathomimetics , and adrenergic antagonists, also called adrenergic blockers or sympatholytics -along with their dosages and uses. (basicmedicalkey.com)
- Intravenous (IV) adrenergic agonists and antagonists are high-alert medications because they can cause significant harm to a patient in the event of a medication error. (basicmedicalkey.com)
- Drugs that stimulate the sympathetic nervous system are called adrenergic agonists, adrenergics, or sympathomimetics because they mimic the sympathetic neurotransmitters norepinephrine and epinephrine. (basicmedicalkey.com)
- Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lookformedical.com)
- Alpha-2 agonists often have a sedating effect and are commonly used as anesthesia enhancers in surgery, as well as in treatment of drug or alcohol dependence . (wikipedia.org)
Blockers6
- At low doses, alpha-adrenergic receptor blockers may be used as monotherapy in the treatment of hypertension. (medscape.com)
- As a result, concurrent diuretic therapy may be required to maintain the hypotensive effects of alpha-receptor blockers. (medscape.com)
- The "intra-operative floppy iris syndrome" cataract surgery complication has been reported in men using alpha-blockers. (urotoday.com)
- The risk of complicated cataract surgery was 14.9% in patients using alpha-blockers, approximately 50% higher than those not receiving this medication (9.5%) (p=0.003). (urotoday.com)
- Beta blockers , which counter some of the effects of noradrenaline by blocking their receptors, are frequently used to treat glaucoma , migraine , and a range of cardiovascular problems. (wikipedia.org)
- Alpha blockers , which counter a different set of noradrenaline effects, are used to treat several cardiovascular and psychiatric conditions. (wikipedia.org)
Selective4
- Thus, polyamines tripitramine (9) and spirotramine (33), among others, were designed, which were shown to be highly selective for muscarinic M(2) and M(1) receptors, respectively. (inrae.fr)
- SSRIs are selective to the 5-HT system but not specific for the different 5-HT receptors. (msdmanuals.com)
- Doxazosin mesylate is a quinazoline compound that is a selective alpha1-adrenergic antagonist. (medscape.com)
- A beta-2 selective adrenergic antagonist. (lookformedical.com)
Beta 2 receptors4
- The beta 2 receptors are found mostly in the smooth muscles of the lung and GI tract, the liver, and the uterine muscle. (basicmedicalkey.com)
- FIG. 15.1 Effects of activation of alpha 1 , alpha 2 , beta 1 , and beta 2 receptors. (basicmedicalkey.com)
- Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. (lookformedical.com)
- The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
Agonist2
- This study was designed to investigate the effects of clonidine and yohimbine, an alpha-2 ( α 2 ) adrenoceptor agonist and antagonist respectively in the tail flick and hot plate tests. (biomedcentral.com)
- The aim of the experiment was to study the role of the noradrenergic receptor system in the NMRs using the receptor agonist clonidine and antagonist yohimbine in the tail flick and hot plate tests, in order to establish whether NMR can be used as animal model for noradrenergic mechanisms in thermal antinociception. (biomedcentral.com)
Nonselective3
- Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
- This is a nonselective alpha-adrenergic blocking agent. (medscape.com)
- This is a nonselective beta-adrenergic receptor blocker. (medscape.com)
Clonidine1
- Management of opioid withdrawal includes the use of other opioids, benzodiazepines and alpha-2 adrenergic receptor antagonist, clonidine. (nih.gov)
Phentolamine1
- Phentolamine, an alpha-adrenergic antagonist (1 microM), reduced sympathetic constriction in controls, but abolished this response in TiO2 exposed rats (max % change -22.3+/-3.1 control, -9.7+/-2.9 TiO2). (cdc.gov)
Stimulation7
- Twenty four hours following exposure, the spinotrapezius muscle was prepared for intravital microscopy and sympathetic nerve stimulation (2, 4, 8, and 16 Hz) was performed. (cdc.gov)
- It may be used to treat excessive beta-receptor stimulation in patients with inoperable metastatic pheochromocytoma. (medscape.com)
- Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart. (aspetjournals.org)
- 1,4,5-IP3 (significant at 10 microM) and both IP4 isomers (significant at 1 microM) increased after alpha-adrenoceptor stimulation, whereas 1,3,4,5,6-IP5 and IP6 remained unaffected. (aspetjournals.org)
- Increased inositol polyphosphate turnover may be involved in the mechanism(s) whereby alpha 1-adrenoceptor stimulation produces an increase in myocardial force of contraction. (aspetjournals.org)
- Stimulation of the beta 1 receptors increases myocardial contractility and heart rate. (basicmedicalkey.com)
- Results from using an in vitro tissue bath technique indicated that propranolol and preferential beta(2)-adrenoceptor antagonists (ICI-118,551 and butoxamine), in a concentration-dependent manner, blocked the relaxation induced by nicotine (100 microM) without affecting the relaxation elicited by transmural nerve stimulation (TNS, 8 Hz). (lookformedical.com)
Propranolol1
- After primary treatment with an alpha-receptor blocker, propranolol hydrochloride may be used as adjunctive therapy if control of tachycardia becomes necessary before or during surgery. (medscape.com)
Blockade3
- The enhanced sensitivity to alpha-adrenergic receptor blockade following TiO2 exposure suggests an augmented responsiveness to tonic sympathetic activity. (cdc.gov)
- Its drug action is transient and alpha-adrenergic blockade incomplete. (medscape.com)
- Leri, F., Flores, J., Rodaros, D., & Stewart, J. (2002) Blockade of stress-induced but not cocaine-induced reinstatement by infusion of noradrenergic antagonists into the bed nucleus of the stria terminalis or the central nucleus of the amygdala. (concordia.ca)
Yohimbine1
- Research has shown that it's mechanisms of action are similar to yohimbine, as it can act as an alpha(2) adrenergic antagonist, thus aiding in fat burning. (anybodysupplements.com)
Postsynaptic2
- By preventing reuptake of 5-HT presynaptically, SSRIs result in more 5-HT to stimulate postsynaptic 5-HT receptors. (msdmanuals.com)
- It inhibits postsynaptic alpha-adrenergic receptors, resulting in the vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure. (medscape.com)
MicroM1
- All effects were antagonized by the alpha 1-adrenoceptor antagonist prazosin (0.1 microM), indicating receptor-mediated effects. (aspetjournals.org)
Presynaptic2
- Presynaptic beta(2)-adrenoceptors mediate nicotine-induced NOergic neurogenic dilation in porcine basilar arteries. (lookformedical.com)
- A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS . (nih.gov)
Muscarinic4
- structure to achieve specific recognition of muscarinic receptors that led to the discovery of methoctramine (2). (inrae.fr)
- which is widely used as a pharmacological tool for muscarinic receptor characterization. (inrae.fr)
- In turn, appropriate structural modifications performed on the structure of methoctramine led to the discovery of new polyamines endowed with high affinity and selectivity for (a). muscarinic receptor subtypes, (b). (inrae.fr)
- Finally, the universal template approach formed the basis for modifying benextramine (1) structure to the design of ligands, which display affinity for acetylcholinesterase and muscarinic M(2) receptors. (inrae.fr)
Epinephrine1
- It is an alpha1- and alpha2-adrenergic blocking agent that blocks circulating epinephrine and norepinephrine action, reducing hypertension that results from catecholamine effects on alpha receptors. (medscape.com)
Norepinephrine2
- [2] "Norepinephrine" is also the international nonproprietary name given to the drug . (wikipedia.org)
- Regardless of how and where it is released, norepinephrine acts on target cells by binding to and activating adrenergic receptors located on the cell surface. (wikipedia.org)
Dopaminergic1
- Other adrenergic receptors are dopaminergic and are located in the renal, mesenteric, coronary, and cerebral arteries. (basicmedicalkey.com)
Noradrenergic2
- Since the tail-flick and hot plate tests mediate the effects at spinal and supraspinal levels respectively, the present study indicates the presence and involvement of noradrenergic receptors in thermal antinociception at spinal and supraspinal levels of the NMR, similar to what has been found in other mammals. (biomedcentral.com)
- To our knowledge, the involvement of the noradrenergic receptor system in antinociception against thermal stimuli has not been previously studied in the NMR. (biomedcentral.com)
Serotonin2
- Unlike first-generation H1- receptor antagonists, they do not cross the bloodbrain barrier and do not bind to cholinergic, serotonin, or alpha-adrenergic re- ceptors.Dell, A. (forextrading-madeeasy.com)
- It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. (nih.gov)
Nitric oxide1
- Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic receptors. (cdc.gov)
Inhibition2
- Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilizatio. (bindingdb.org)
- Antagonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization. (bindingdb.org)
Activate3
- Only dopamine can activate these receptors. (basicmedicalkey.com)
- Alternatively, one can admit that CEC is able to inhibit alpha-2 autoreceptors, which causes an increase of the transmitter release, and to activate a nonadrenergic inhibitory receptor thus causing a reduction of the transmitter release. (unesp.br)
- Drugs that selectively bind to and activate beta-adrenergic receptors. (lookformedical.com)
Medications4
- Alpha-blocker medications are the first line of therapy for men with these urinary symptoms. (urotoday.com)
- If possible, alpha blocker medications should be discontinued prior to eye surgery in older patients. (urotoday.com)
- As alpha-blocker medications are the first line of therapy for men with LUTS, these reports of IFIS led the Food and Drug Administration, American Urological Association, American Academy of Ophthalmology, and American Society of Cataract and Refractive Surgery to issue statements alerting physicians and patients to potential difficulties during cataract surgery in patients using alpha-1 blocker therapy [7,8,9]. (urotoday.com)
- Alpha-receptor antagonist medications potentially interfere with iris muscle dilation, resulting in difficult lens removal and possibly increasing complications. (urotoday.com)
Prevalence1
- INT RODUCTIO N: Th e eld erly h ypert en si ve pa ti ent s of ten h aveincreased prevalence of cardiometabolic risk factors and their attendantco-morbidities. (bvsalud.org)
Blocker4
- Preoperatively, prepare patients with pheochromocytomas by treating them with an alpha-blocker or a tyrosine hydroxylase inhibitor, such as metyrosine, for 1-2 weeks, after which administration of a beta-blocker can be considered. (medscape.com)
- This is a long-acting adrenergic alpha-receptor blocker that can produce and maintain a chemical sympathectomy. (medscape.com)
- To assess the frequency of cataract surgery complications arising from alpha-blocker therapy in a large patient population. (urotoday.com)
- The purpose of this study was to assess the impact of alpha-blocker therapy on complications during cataract surgery in a large patient population. (urotoday.com)
Sympathetic2
- Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in heart rate, sympathetic tone, and activity of the renin aldosterone system. (biopsychiatry.com)
- The alpha 2 receptors are located in the postganglionic sympathetic nerve endings. (basicmedicalkey.com)
Anxiety2
- They stimulate 5-HT 1 receptors, with antidepressant and anxiolytic effects, but they also stimulate 5-HT 2 receptors, commonly causing anxiety, insomnia, and sexual dysfunction, and 5-HT 3 receptors, commonly causing nausea and headache. (msdmanuals.com)
- For reasons that are still unclear, some Alpha-2 drugs, such as guanfacine , have also been shown to be effective in the treatment of anxiety disorders and ADHD . (wikipedia.org)
Vasoconstriction1
- It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. (lookformedical.com)
Drugs1
- Sulfonylureas are generally ef- fective, safe, and inexpensive (generically available) drugs and, along with metformin, are mainstays of treatment for type 2 diabetes. (forextrading-madeeasy.com)
Contraction2
- The increase in the force of contraction started at 2 min. (aspetjournals.org)
- The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. (lookformedical.com)
Primarily2
- The beta 1 receptors are located primarily in the heart but are also found in the kidney. (basicmedicalkey.com)
- It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS. (lookformedical.com)
Increases1
- When these receptors are stimulated, the vessels dilate and blood flow increases. (basicmedicalkey.com)
Widely2
- A study published in 2005 described a new clinical entity, the "intra-operative floppy iris syndrome" (IFIS), and suggested that this syndrome was associated with tamsulosin, a drug used widely for the treatment of lower urinary tract symptoms (LUTS) due to benign prostate enlargement [2]. (urotoday.com)
- A widely used non-cardioselective beta-adrenergic antagonist. (lookformedical.com)
Diseases2
- These results highlight the urgent need for prospective trials testing whether prophylactic use of α1-AR antagonists ameliorates diseases associated with cytokine storm syndrome, such as COVID-19. (stanford.edu)
- Due to these unique characteristics, researchers have been bio prospecting NMRs as research animal models for nociception with the aim to further understand mechanisms involved in various biological diseases affecting humans [ 2 , 3 , 5 ]. (biomedcentral.com)
Nerve2
- Transmitters are inactivated by (1) reuptake of the transmitter back into the neuron (nerve cell terminal), (2) enzymatic transformation or degradation, and (3) diffusion away from the receptor. (basicmedicalkey.com)
- Results of double-labeling studies indicated that beta(2)-adrenoceptor immunoreactivities and NADPH diaphorase reactivities were colocalized in the same nerve fibers in basilar and middle cerebral arteries. (lookformedical.com)
Weeks1
- Moreover, the patient must have psychosis for at least 2 weeks without a mood disorder. (medscape.com)
Prostate1
- The alpha-adrenergic receptors are located in the blood vessels, eyes, bladder, and prostate. (basicmedicalkey.com)
Relaxation1
- In contrast, preferential beta(1)-adrenoceptor antagonists (atenolol and CGP-20712A) did not affect either nicotine- or TNS-induced relaxation. (lookformedical.com)
Mediate1
- The four main receptors are alpha 1 , alpha 2 , beta 1 , and beta 2 , which mediate the major responses described in Table 15.1 and illustrated in Fig. 15.1 . (basicmedicalkey.com)
Gastrointestinal1
- They act on one or more adrenergic receptor sites located in the effector cells of muscles such as the heart, bronchiole walls, gastrointestinal (GI) tract, urinary bladder, and ciliary muscles of the eye. (basicmedicalkey.com)
Syndrome1
- We previously demonstrated that alpha-1 adrenergic receptor (α1-AR) antagonists can prevent cytokine storm syndrome in mice. (stanford.edu)
Affinity1
- As a matter of fact, the insertion of different pharmacophores onto the polymethylene tetraamine backbone can tune both affinity and selectivity for any given receptor. (inrae.fr)
Effect2
- The FDA considers the risk for IFIS to be a class effect for alpha-1 adrenergic receptor antagonists [8,9]. (urotoday.com)
- The present study was undertaken to look for the effect of chloroethylclonidine (CEC) on prejunctional alpha-2 autoreceptors of the canine saphenous vein. (unesp.br)
Trials1
- Risk of bias will be assessed using the Cochrane risk-of-bias tool for randomised trials (RoB 2), Risk of Bias in Non-randomised Studies of Interventions (ROBINS-I), and The Joanna Briggs Institute Critical Appraisal Checklist for Quasi-Experimental Studies and The Joanna Briggs Institute Critical Appraisal Checklist for Qualitative Research (CASP), depending on the study type. (bvsalud.org)
Type2
- G(i) proteins, and (c). muscle-type nicotinic receptors. (inrae.fr)
- The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS. (lookformedical.com)
Block1
- Rauwolscine (1mg) Rauwolscine is an alpha-receptor antagonist that can block the action of receptors responsible for stopping fat breakdown. (anybodysupplements.com)
Main1
- Federated across two ARD cohorts, our main result shows that patients using α1-AR antagonists, as compared to nonusers, had a 40% relative risk reduction for ventilation and dying (p=0.014). (stanford.edu)