Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.
Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of ACETYLCHOLINE, and drugs that affect the survival of cholinergic neurons. The term cholinergic agents is sometimes still used in the narrower sense of MUSCARINIC AGONISTS, although most modern texts discourage that usage.
A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
An alkaloid obtained from the betel nut (Areca catechu), fruit of a palm tree. It is an agonist at both muscarinic and nicotinic acetylcholine receptors. It is used in the form of various salts as a ganglionic stimulant, a parasympathomimetic, and a vermifuge, especially in veterinary practice. It has been used as a euphoriant in the Pacific Islands.
A toxic alkaloid found in Amanita muscaria (fly fungus) and other fungi of the Inocybe species. It is the first parasympathomimetic substance ever studied and causes profound parasympathetic activation that may end in convulsions and death. The specific antidote is atropine.
Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Receptor, Muscarinic M1
A specific subtype of muscarinic receptor that has a high affinity for the drug PIRENZEPINE. It is found in the peripheral GANGLIA where it signals a variety of physiological functions such as GASTRIC ACID secretion and BRONCHOCONSTRICTION. This subtype of muscarinic receptor is also found in neuronal tissues including the CEREBRAL CORTEX and HIPPOCAMPUS where it mediates the process of MEMORY and LEARNING.
alpha7 Nicotinic Acetylcholine Receptor
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
Receptor, Muscarinic M3
A form of phagocyte bactericidal dysfunction characterized by unusual oculocutaneous albinism, high incidence of lymphoreticular neoplasms, and recurrent pyogenic infections. In many cell types, abnormal lysosomes are present leading to defective pigment distribution and abnormal neutrophil functions. The disease is transmitted by autosomal recessive inheritance and a similar disorder occurs in the beige mouse, the Aleutian mink, and albino Hereford cattle.
The front part of the hindbrain (RHOMBENCEPHALON) that lies between the MEDULLA and the midbrain (MESENCEPHALON) ventral to the cerebellum. It is composed of two parts, the dorsal and the ventral. The pons serves as a relay station for neural pathways between the CEREBELLUM to the CEREBRUM.
Dose-Response Relationship, Drug
An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)
Parasympathetic Nervous System
The craniosacral division of the autonomic nervous system. The cell bodies of the parasympathetic preganglionic fibers are in brain stem nuclei and in the sacral spinal cord. They synapse in cranial autonomic ganglia or in terminal ganglia near target organs. The parasympathetic nervous system generally acts to conserve resources and restore homeostasis, often with effects reciprocal to the sympathetic nervous system.
Nerve fibers liberating acetylcholine at the synapse after an impulse.
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in URINARY INCONTINENCE, in MOTION SICKNESS, as an antispasmodic, and as a mydriatic and cycloplegic.
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
A glandular epithelial cell or a unicellular gland. Goblet cells secrete MUCUS. They are scattered in the epithelial linings of many organs, especially the SMALL INTESTINE and the RESPIRATORY TRACT.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
Neurotoxic proteins from the venom of the banded or Formosan krait (Bungarus multicinctus, an elapid snake). alpha-Bungarotoxin blocks nicotinic acetylcholine receptors and has been used to isolate and study them; beta- and gamma-bungarotoxins act presynaptically causing acetylcholine release and depletion. Both alpha and beta forms have been characterized, the alpha being similar to the large, long or Type II neurotoxins from other elapid venoms.
A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
In about 250 species of electric fishes, modified muscle fibers forming disklike multinucleate plates arranged in stacks like batteries in series and embedded in a gelatinous matrix. A large torpedo ray may have half a million plates. Muscles in different parts of the body may be modified, i.e., the trunk and tail in the electric eel, the hyobranchial apparatus in the electric ray, and extrinsic eye muscles in the stargazers. Powerful electric organs emit pulses in brief bursts several times a second. They serve to stun prey and ward off predators. A large torpedo ray can produce of shock of more than 200 volts, capable of stunning a human. (Storer et al., General Zoology, 6th ed, p672)
Receptor, Muscarinic M2
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
Vasoactive Intestinal Peptide
A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).
Therapeutic introduction of ions of soluble salts into tissues by means of electric current. In medical literature it is commonly used to indicate the process of increasing the penetration of drugs into surface tissues by the application of electric current. It has nothing to do with ION EXCHANGE; AIR IONIZATION nor PHONOPHORESIS, none of which requires current.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 126.96.36.199.
Adrenergic alpha-2 Receptor Agonists
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Serotonin 5-HT2 Receptor Agonists
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
The function of opposing or restraining the excitation of neurons or their target excitable cells.
Protein Kinase C
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
Serotonin 5-HT1 Receptor Agonists
Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.
Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
Adenosine A1 Receptor Agonists
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Rats, Inbred Strains
Excitatory Postsynaptic Potentials
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
Adrenergic alpha-1 Receptor Agonists
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
Cannabinoid Receptor Agonists
Receptors, Opioid, mu
Adenosine A3 Receptor Agonists
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
Receptors, Opioid, kappa
Receptors, Opioid, delta
Serotonin 5-HT4 Receptor Agonists
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Receptors, Dopamine D2
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Modulation of long-term synaptic depression in visual cortex by acetylcholine and norepinephrine. (1/652)In a slice preparation of rat visual cortex, we discovered that paired-pulse stimulation (PPS) elicits a form of homosynaptic long-term depression (LTD) in the superficial layers when carbachol (CCh) or norepinephrine (NE) is applied concurrently. PPS by itself, or CCh and NE in the absence of synaptic stimulation, produced no lasting change. The LTD induced by PPS in the presence of NE or CCh is of comparable magnitude with that obtained with prolonged low-frequency stimulation (LFS) but requires far fewer stimulation pulses (40 vs 900). The cholinergic facilitation of LTD was blocked by atropine and pirenzepine, suggesting involvement of M1 receptors. The noradrenergic facilitation of LTD was blocked by urapidil and was mimicked by methoxamine, suggesting involvement of alpha1 receptors. beta receptor agonists and antagonists were without effect. Induction of LTD by PPS was inhibited by NMDA receptor blockers (completely in the case of NE; partially in the case of CCh), suggesting that one action of the modulators is to control the gain of NMDA receptor-dependent homosynaptic LTD in visual cortex. We propose that this is a mechanism by which cholinergic and noradrenergic inputs to the neocortex modulate naturally occurring receptive field plasticity. (+info)
Metrifonate increases neuronal excitability in CA1 pyramidal neurons from both young and aging rabbit hippocampus. (2/652)The effects of metrifonate, a second generation cholinesterase inhibitor, were examined on CA1 pyramidal neurons from hippocampal slices of young and aging rabbits using current-clamp, intracellular recording techniques. Bath perfusion of metrifonate (10-200 microM) dose-dependently decreased both postburst afterhyperpolarization (AHP) and spike frequency adaptation (accommodation) in neurons from young and aging rabbits (AHP: p < 0.002, young; p < 0.050, aging; accommodation: p < 0.024, young; p < 0.001, aging). These reductions were mediated by muscarinic cholinergic transmission, because they were blocked by addition of atropine (1 microM) to the perfusate. The effects of chronic metrifonate treatment (12 mg/kg for 3 weeks) on CA1 neurons of aging rabbits were also examined ex vivo. Neurons from aging rabbits chronically treated with metrifonate had significantly reduced spike frequency accommodation, compared with vehicle-treated rabbits. Chronic metrifonate treatment did not result in a desensitization to metrifonate ex vivo, because bath perfusion of metrifonate (50 microM) significantly decreased the AHP and accommodation in neurons from both chronically metrifonate- and vehicle-treated aging rabbits. We propose that the facilitating effect of chronic metrifonate treatment on acquisition of hippocampus-dependent tasks such as trace eyeblink conditioning by aging subjects may be caused by this increased excitability of CA1 pyramidal neurons. (+info)
Influence of nitric oxide modulators on cholinergically stimulated hormone release from mouse islets. (3/652)1. We have investigated, with a combined in vitro and in vivo approach, the influence on insulin and glucagon release stimulated by the cholinergic, muscarinic agonist carbachol of different NO modulators, i.e. the nitric oxide synthase (NOS) inhibitors NG-nitro-L-arginine methyl ester (L-NAME), NG-monomethyl-L-arginine (L-NMMA) and 7-nitroindazole as well as the intracellular NO donor hydroxylamine. 2. At basal glucose (7 mM) carbachol dose-dependently stimulated insulin release from isolated islets with a half-maximal response at approximately 1 microM of the agonist. In the presence of 5 mM L-NAME (a concentration that did not influence basal insulin release) the insulin response was markedly increased along the whole dose-response curve and the threshold for carbachol stimulation was significantly lowered. 3. Carbachol-stimulated islets displayed an increased insulin release and a suppressed glucagon release in the presence of L-NAME, L-NMMA or 7-nitroindazole. Significant suppression of glucagon release (except for L-NAME) was achieved at lower concentrations (approximately 0.1-0.5 mM) of the NOS inhibitors than the potentiation of insulin release (1.0-5.0 mM). The intracellular NO donor hydroxylamine dose-dependently inhibited carbachol-induced insulin release but stimulated glucagon release only at a low concentration (3 microM). 4. In islets depolarized with 30 mM K+ in the presence of the KATP channel opener diazoxide, NOS inhibition by 5 mM L-NAME still markedly potentiated carbachol-induced insulin release (although less so than in normal islets) and suppressed glucagon release. 5. In vivo pretreatment of mice with L-NAME was followed by a markedly increased insulin release and a reduced glucagon release in response to an i.v. injection of carbachol. 6. The data suggest that NO is a negative modulator of insulin release but a positive modulator of glucagon release induced by cholinergic muscarinic stimulation. These effects were also evident in K+ depolarized islets and thus NO might exert a major influence on islet hormone secretion independently of membrane depolarization events. (+info)
Miniglucagon (glucagon 19-29), a potent and efficient inhibitor of secretagogue-induced insulin release through a Ca2+ pathway. (4/652)Using the MIN6 B-cell line, we investigated the hypothesis that miniglucagon, the C-terminal () fragment processed from glucagon and present in pancreatic A cells, modulates insulin release, and we analyzed its cellular mode of action. We show that, at concentrations ranging from 0.01 to 1000 pM, miniglucagon dose-dependently (ID50 = 1 pM) inhibited by 80-100% the insulin release triggered by glucose, glucagon, glucagon-like peptide-1-(7-36) amide (tGLP-1), or glibenclamide, but not that induced by carbachol. Miniglucagon had no significant effects on cellular cAMP levels. The increase in 45Ca2+ uptake induced by depolarizing agents (glucose or extracellular K+), by glucagon, or by the Ca2+channel agonist Bay K-8644 was blocked by miniglucagon at the doses active on insulin release. Electrophysiological experiments indicated that miniglucagon induces membrane hyperpolarization, probably by opening potassium channels, which terminated glucose-induced electrical activity. Pretreatment with pertussis toxin abolished the effects of miniglucagon on insulin release. It is concluded that miniglucagon is a highly potent and efficient inhibitor of insulin release by closing, via hyperpolarization, voltage-dependent Ca2+ channels linked to a pathway involving a pertussis toxin-sensitive G protein. (+info)
Cholinergic and GABAergic regulation of nitric oxide synthesis in the guinea pig ileum. (5/652)Nitric oxide (NO) synthesis was examined in intact longitudinal muscle-myenteric plexus preparations of the guinea pig ileum by determining the formation of [3H]citrulline during incubation with [3H]arginine. Spontaneous [3H]citrulline production after 30 min was 80-90 dpm/mg, which constituted approximately 1% of the tissue radioactivity. Electrical stimulation (10 Hz) led to a threefold increase in [3H]citrulline formation. Removal of calcium from the medium or addition of NG-nitro-L-arginine strongly inhibited both spontaneous and electrically induced production of [3H]citrulline. TTX reduced the electrically induced but not spontaneous [3H]citrulline formation. The electrically induced formation of [3H]citrulline was diminished by (+)-tubocurarine and mecamylamine and enhanced by scopolamine, which suggests that endogenous ACh inhibits, via muscarinic receptors, and stimulates, via nicotinic receptors, the NO synthesis in the myenteric plexus. The GABAA receptor agonist muscimol and GABA also reduced the electrically evoked formation of [3H]citrulline, whereas baclofen was without effect. Bicuculline antagonized the inhibitory effect of GABA. It is concluded that nitrergic myenteric neurons are equipped with GABAA receptors, which mediate inhibition of NO synthesis. (+info)
Purinergic and cholinergic agonists induce exocytosis from the same granule pool in HT29-Cl.16E monolayers. (6/652)Several secretagogues induce mucin secretion in epithelial monolayers, as determined by measuring released granule contents. To assess whether different agonists act on the same granule pool, capacitance changes in intact monolayers of the goblet cell line HT29-Cl.16E were measured by a novel impedance method. Apical ATP (purinergic agonist) and basolateral carbachol (cholinergic agonist) induce rapid exocytosis with maximal capacitance changes within 3 min. The maximal levels of exocytosis that can be induced by optimal concentrations of either agonist are the same and produce a 30-40% increase in total monolayer capacitance. When ATP and carbachol are applied simultaneously, the magnitude of exocytosis is unchanged from the single-secretagogue level. The recovery of capacitance to baseline (endocytosis) is significantly faster after ATP stimulation than after carbachol stimulation. When ATP and carbachol are applied sequentially at doses that give maximal exocytosis, the magnitude of the capacitance increase produced by the second secretagogue is less than or equal to that of the capacitance decrease during the recovery period. Together, these data suggest that purinergic and cholinergic agonists act on the same granule pool. (+info)
Immunolocalization of muscarinic and VIP receptor subtypes and their role in stimulating goblet cell secretion. (7/652)PURPOSE: To determine the subtypes of cholinergic muscarinic receptors and receptors for vasoactive intestinal peptide (VIP) present in rat conjunctival goblet cells and whether cholinergic agonists and VIP stimulate goblet cell secretion. METHODS: Immunofluorescence studies were performed using antibodies against the m1, m2, and m3 muscarinic receptor subtypes and VIP receptors 1 and 2 (VIPR1 and VIPR2). The lectin Ulex europeus agglutinin I was used to measure glycoconjugate secretion, the index of secretion, from goblet cells in an enzyme-linked lectin assay. In this assay, pieces of conjunctiva were placed on filter paper and incubated for 15 to 120 minutes, with or without increasing concentrations of the cholinergic agonist carbachol or VIP. The muscarinic antagonist atropine and the muscarinic receptor-subtype-selective antagonists pirenzepine (M1), gallamine (M2), and 4-4-diphenylacetoxy-N-(2-chloroethyl)-piperidine hydrochloride (4-DAMP mustard; M3) were incubated with carbachol to determine specificity of receptor activation. RESULTS: Immunoreactivity to M2 and M3 receptors was found on goblet cell membranes subjacent to the secretory granules. Immunoreactivity to M1 receptor was not on goblet cells but was on the stratitfied squamous cells. Immunoreactivity to VIPR2 was found on goblet cells with a localization similar to that of the M2 and M3 receptors. VIPR1 was not found on goblet cells or on the stratified squamous cells. Carbachol and VIP induced a time- and concentration-dependent stimulation of glycoconjugate secretion. Carbachol, at 10(-4) M, induced a threefold increase in glycoconjugate secretion, which was completely inhibited by atropine (10(-5) M). Carbachol-induced secretion was inhibited 54% +/- 8% by pirenzepine (10(-5) M), 69% +/- 14% by gallamine (10(-5) M), and 72% +/- 11% by 4-DAMP mustard (10(-5) M). A twofold increase in glycoconjugate secretion was obtained with VIP at 10(-8) M. CONCLUSIONS: Cholinergic agonists, through M2 and/or M3 muscarinic receptors, and VIP, through VIPR2, regulate conjunctival goblet cell secretion, suggesting that goblet cell secretion in vivo is under the control of parasympathetic nerves. (+info)
Modulation of inhibitory synaptic potentials in the piriform cortex. (8/652)Modulation of inhibitory synaptic potentials in the piriform cortex. Intracellular recordings from pyramidal neurons in brain slice preparations of the piriform cortex were used to test results from a computational model about the effects of cholinergic agonists on inhibitory synaptic potentials induced by stimulation of afferent fibers in layer Ia and association/intrinsic fibers in layer Ib. A simple model of piriform cortex as an associative memory was used to analyze how suppression of inhibitory synaptic transmission influenced performance of the network. Levels of suppression of excitatory synaptic transmission were set at levels determined in previous experimental work. Levels of suppression of inhibitory synaptic transmission were then systematically varied within the model. This modeling work demonstrated that suppression of inhibitory synaptic transmission in layer Ib should be stronger than suppression of inhibitory synaptic transmission in layer Ia to keep activity levels high enough for effective storage. Experimental data showed that perfusion of the cholinergic agonist carbachol caused a significant suppression of inhibitory postsynaptic potentials (IPSPs) in the pyramidal neurons that were induced by stimulation of layer Ib, with a weaker effect on IPSPs induced by stimulation of layer Ia. As previously described, carbachol also selectively suppressed excitatory postsynaptic potentials (EPSPs) elicited by intrinsic but not afferent fiber stimulation. The decrease in amplitude of IPSPs induced by layer Ib stimulation did not appear to be directly related to the decrease in EPSP amplitude induced by layer Ib stimulation. The stimulation necessary to induce neuronal firing with layer Ia stimulation was reduced in the presence of carbachol, whereas that necessary to induce neuronal firing with layer Ib stimulation was increased, despite the depolarization of resting membrane potential. Thus physiological data on cholinergic modulation of inhibitory synaptic potentials in the piriform cortex is compatible with the functional requirements determined from computational models of piriform cortex associative memory function. (+info)
Adrenergic and cholinergic control on the heart in rat ontogenesis | SpringerLink
JoVE Author Search: Caban B
Carbachol - యొక్క ఉపయోగాలు, మోతాదు, దుష్ప్రభావాలు, ప్రయోజనాలు, పరస్పర చర్యలు మరియు హెచ్చరిక - Carbachol in Telugu
Carbachol- యొక్క ఉపయోగాలు, మోతాదు, దుష్ప్రభావాలు, ప్రయోజనాలు, పరస్పర చర్యలు మరియు హెచ్చరికను కనుగొనండి
Mechanisms of release of atrial natriuretic factor. I. Effect of several agonists and steroids on its release by atrial minces
The effect that several substances may have on ANF release by atrial slices and on its tissular content was investigated. alpha- and beta-adrenergic and cholinergic agonists, vasopressin, met-enkephaline, dexamethasone and DOC, in concentration ranging from 10(-4) to 10(-8) M, were added into the in …
Pesquisa | Portal Regional da BVS
Depolarization-induced suppression of inhibition (DSI) is a prevailing form of endocannabinoid signalling. However, several discrepancies have arisen regarding the roles played by the two major brain endocannabinoids, 2-arachidonoylglycerol (2-AG) and anandamide, in mediating DSI. Here we studied endocannabinoid signalling in the prefrontal cortex (PFC), where several components of the endocannabinoid system have been identified, but endocannabinoid signalling remains largely unexplored. In voltage clamp recordings from mouse PFC pyramidal neurons, depolarizing steps significantly suppressed IPSCs induced by application of the cholinergic agonist carbachol. DSI in PFC neurons was abolished by extra- or intracellular application of tetrahydrolipstatin (THL), an inhibitor of the 2-AG synthesis enzyme diacylglycerol lipase (DAGL). Moreover, DSI was enhanced by inhibiting 2-AG degradation, but was unaffected by inhibiting anandamide degradation. THL, however, may affect other enzymes of lipid ...
c-AS - carbachol-induced active sleep | AcronymAttic
How is carbachol-induced active sleep abbreviated? c-AS stands for carbachol-induced active sleep. c-AS is defined as carbachol-induced active sleep rarely.
Spatio-temporal patterns of CCh-induced [Ca2+]i transie | Open-i
Spatio-temporal patterns of CCh-induced [Ca2+]i transients. The x-y confocal Ca2+ imaging was performed at 32 Hz (A and B), 40 Hz (C), 44 Hz (D) and 30 Hz
Nursing Pharmacology: Cholinergic Pharmacology
Stoelting, R.K., Anticholinesterase Drugs and Cholinergic Agonists, in Pharmacology and Physiology in Anesthetic Practice, Lippincott-Raven Publishers, 1999, 224-237; Taylor, P. Anticholinesterase Agents, In, Goodman and Gillmans The Pharmacologial Basis of Therapeutics,(Hardman, J.G, Limbird, L.E, Molinoff, P.B., Ruddon, R.W, and Gilman, A.G.,eds) TheMcGraw-Hill Companies, Inc.,1996, pp.161-174.. ...
Carbachol Manufacturer,Carbachol Supplier,Exporter
Carbachol ophthalmic and Ceron-DM Drops Drug Interactions - Drugs.com
A Moderate Drug Interaction exists between carbachol ophthalmic and Ceron-DM Drops. View detailed information regarding this drug interaction.
buy viagra walmart iphone was
In Chapter 11, we discussed the development of alpha-7-nicotinic cholinergic agonists as a novel therapeutic strategy for schizophrenia. 10.
Isopto Carbachol - Side Effects, Uses, Dosage, Overdose, Pregnancy, Alcohol | RxWiki
Cyclic nucleotides in muscarinic regulation of DNA and RNA polymerase activity in cultured corneal epithelial cells of the...
TY - JOUR. T1 - Cyclic nucleotides in muscarinic regulation of DNA and RNA polymerase activity in cultured corneal epithelial cells of the rabbit. AU - Colley, A. M.. AU - Cavanagh, Harrison D. AU - Drake, L. A.. AU - Law, M. L.. N1 - Funding Information: ACKNOWLEDGMENTS This work was supported by National Eye Institute Research Grant No. EY04604 and a Departmental grant from Research to Prevent Blindness. The authors gratefully acknowledge the technical assistance o f Mr. Neil Matthews i n photography and animal care and the administrative and clerical assistance of Mrs. Edith Barron, Mrs. Cynthia Hale, and Mrs. LaDonna Hampton.. PY - 1985. Y1 - 1985. N2 - DNA and RNA polymerase activities in the purified nuclear fraction from cultured rabbit corneal epithelial cells were assayed over a range of substrate (labeled dTTP or UTP) concentrations using calf thymus DNA as template. Effects of carbamylcholine on polymerase activities were evaluated over a range of drug concentrations including those ...
Tao living in exocytosis.
Therefore, it is also possible to modify our algorithm to study the coupling mechanisms between exocytosis and endocytosis in the future. Combinatorial microscopy. Google Scholar Employing FM fluorescence imaging, basolateral exocytosis was observed in dispersed rat pancreatic acini after supramaximal CCK or carbachol stimulation; and more remarkably, also after treatment with clinically-relevant concentrations of alcohol and putative alcohol metabolites followed by physiologic CCK or carbachol stimulation 8, 9, 28thus simulating alcoholic pancreatitis. AIP Conf. In summary, we have developed a software platform for the identification and spatiotemporal analysis of vesicle fusion events obtained by TIRF microscopy.. ...
Xerostomia is a subjective sensation of dry mouth, this is a common symptom particularly in older adults and has a variety of causes. Pilocarpine is a cholinergic agonist that non-selectively binds to muscarinic receptors in smooth muscles in the gastrointestinal, urinary and pulmonary systems and stimulates the production of secretions from the salivary and sweat [read the full story…]. ...
Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine<...
TY - JOUR. T1 - Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine. AU - Nowak, Thomas V.. AU - Harrington, Bonnie. PY - 1985/1/1. Y1 - 1985/1/1. N2 - Proximal and distal rat small intestine was cut into strips measuring 6.0 × 10.0 mm. Strips cut along the oral-caudal axis were called longitudinal strips, whereas those cut 90° to that axis were called circular strips. Stress in circular and longitudinal muscle strips was measured continuously as they were superf used with acetylcholine, carbamylcholine, methacholine, bethanechol, or physostigmine. Resting stress during stretch, acetylcholine-stimulated active stress, and total stress were determined. Proximal circular muscle was five times as sensitive to acetylcholine as distal circular muscle (p , 0.05); proximal longitudinal muscle was 2.8 times as sensitive to bethanechol as distal muscle (p , 0.05). Resting, active, and total stress were similar in proximal and distal muscle, but circular muscle ...
Optical imaging of Ca2+-evoked fluid secretion by murine nasal submucosal gland serous acinar cells - Lee - 2007 - The Journal...
The molecular identities of the pathways that mediate K+ and Cl− effluxes in serous acinar cells are unknown. CFTR mRNA is expressed in these cells, and immunocytochemistry revealed it to be present near the apical membrane. To examine the role of CFTR in Ca2+-evoked fluid secretion, we employed cells from the cftrtm1Unc−/− mouse and we pharmacologically inhibited CFTR in WT mouse cells. The results demonstrated that mouse nasal acinar cells from both WT and cftrtm1Unc−/− mice, as well as WT cells treated with CFTRinh172, all exhibited similar rates of Cl− efflux in response to muscarinic stimulation. Isolated intact submucosal glands from CF individuals that lack functional CFTR can secrete fluid in response to cholinergic agonists (Joo et al. 2002a), and it was recently shown that intact glands in WT and cftrtm1Unc−/− mice trachea secrete fluid in response to CCh at similar rates (Ianowski et al. 2007). It has remained unclear if cholinergic-induced fluid secretion in CF glands ...
Role of Neurotrophins and Neurotrophin Receptors in Rat Conjunctival Goblet Cell Secretion and Proliferation | IOVS | ARVO...
For immunofluorescence microscopy, the eyes were enucleated with the lids intact and fixed in 4% formaldehyde in phosphate-buffered saline (PBS; 145 mM NaCl, 7.3 mM Na2HPO4, and 2.7 mM NaH2PO4 [pH 7.2]), for 4 hours at 4°C. The eyes were then rinsed in 5% sucrose dissolved in PBS, placed overnight in 30% sucrose dissolved in PBS at 4°C, embedded in OCT, and frozen. Cryostat sections (6 μm) were placed on slides (Colorfrost/Plus; Fisher Scientific, Pittsburgh, PA) and kept at −20°C until use. Cultured goblet cells (CGCs) grown on glass coverslips were fixed in absolute methanol. Tissue sections and CGCs were then washed in PBS and blocked in PBS containing 1% bovine serum albumin, 4% goat serum, and 0.2% to 0.3% Triton X-100. The NT antibodies (NGF, BDNF, NT3, and NT4) were used at a dilution of 1:800. The NTr antibodies (TrkA, TrkB, TrkC, and p75) were used at a dilution of 1:200. All antibodies were diluted in PBS containing 0.3% Triton X-100 and incubated for 48 hours at 4°C. The ...
Akinesia, motor oscillations and the pedunculopontine nucleus in rats and men. - Department of Physiology, Anatomy and Genetics...
carbachol ophthalmic | PeaceHealth
Pancreas. Symptoms of the disease | WikBio
The pancreas is a mixed gland secretion (external or internal or digestive and insulin) that is in the highest part of the deep abdominal cavity behind the stomach. The pancreas is located in a transverse position with a head, body and tail. Its internal structure is clustered and each of the grains corresponds to a secretory gland acinus.
Role of the T-type Ca(2+) current on the contractile performance of guinea pig detrusor smooth muscle - UCL Discovery
UCL Discovery is UCLs open access repository, showcasing and providing access to UCL research outputs from all UCL disciplines.
NeuroElectro :: Data table 96
Values are means ± SE. Cholinergic responses evoked by bath application of carbachol (10 μM for 5 min) in CA3 pyramidal neurons. Boldface numbers indicate P , 0.05 for carbachol-induced effects within individual cell types (repeated-measures ANOVA with post-tests: baseline, carbachol, and wash). Asterisks indicate P , 0.01 when compared with values in wild-type neurons (one-way ANOVA with post-tests). ...
Cholinergic receptor - RightDiagnosis.com
Cholinergic receptor information including symptoms, causes, diseases, symptoms, treatments, and other medical and health issues.
Cholinergic inhibition of slow delayed-rectifier K+ current in guinea pig sino-atrial node is not mediated by muscarinic...
We studied the effects of cholinergic agonists on slow delayed-rectifier K+ current (IKs) in isolated cells from the sino-atrial node (SAN) region of guinea pig heart, using patch-clamp procedures. Carbachol (5 nM to 10 microM) inhibited IKs in guinea pig SAN cells in the absence of previous beta-adrenergic stimulation and in cells pretreated with 8-(4-chlorophenylthio)-cAMP. Neither the muscarinic antagonist atropine nor the nicotinic antagonist hexamethonium antagonized carbachol inhibition of the current. Similar results were obtained with other cholinergic agonists. Cholinergic stimulation of the muscarinic K+ current was successfully antagonized by atropine in SAN cells where inhibition of IKs persisted. Therefore, the lack of antagonist effects on inhibition of IKs cannot be attributed to either an absence of muscarinic cholinoceptors on SAN cells or a loss of antagonist activity under our experimental conditions. These data demonstrate that cholinergic agonists, including the endogenous ...
Cholinergic modulation of MEG resting-state oscillatory activity in Parkinsons disease related dementia<...
TY - JOUR. T1 - Cholinergic modulation of MEG resting-state oscillatory activity in Parkinsons disease related dementia. AU - Bosboom, J.L.W.. AU - Stoffers, D.. AU - Stam, C.J.. AU - Berendse, H.W.. AU - Wolters, E.C.. PY - 2009. Y1 - 2009. U2 - 10.1016/j.clinph.2009.03.004. DO - 10.1016/j.clinph.2009.03.004. M3 - Article. C2 - 19386543. VL - 120. SP - 910. EP - 915. JO - Clinical Neurophysiology. JF - Clinical Neurophysiology. SN - 1388-2457. IS - 5. ER - ...
emulsifiable concentrates abamectin, emulsifiable concentrates abamectin Suppliers and Manufacturers at Alibaba.com
Alibaba.com offers 87 emulsifiable concentrates abamectin products. About 8% of these are Insecticide. A wide variety of emulsifiable concentrates abamectin options are available to you,
IO-CHOL - Surgitech Innovation Pvt. Ltd.
Natural Veterinary Services FL | Anesthesia-Free Dental Cleaning
Our Mobile Vet Unit visits pet stores in Florida. Natural Veterinary Services FL Offers Holistic Treatments Tests for Pets. A+ Angies List 5-Star Reviews
Both drugs are agonists are nicotinic cholinergic receptors ... Robert L. Metcalf (2007), "Insect Control", Ullmann's ... Nicotine increases cholinergic signalling and adrenergic signalling in the case of colon cancer, thereby impeding apoptosis ( ... Nicotine acts as an agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits ( ... This nicotine-induced dopamine release occurs at least partially through activation of the cholinergic-dopaminergic reward link ...
Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic GABAergic Glycinergic Histaminergic Monoaminergic ... Examples include melatonin receptor agonists and melatonin receptor antagonists. ...
Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. Both are direct-acting ... Muscarine mimics the function of the natural neurotransmitter acetylcholine in the muscarinic part of the cholinergic nervous ... Muscarinic agonists are used as drugs in treating glaucoma, postoperative ileus, congenital megacolon, urinary retention and ... Inocybe and Clitocybe contain muscarine concentrations up to 1.6%. Muscarine is a nonselective agonist of the muscarinic ...
Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic GABAergic Glycinergic Melatonergic Monoaminergic Opioidergic ... Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine ...
Thus it is classified as a cholinergic agonist. It is primarily used for various ophthalmic purposes, such as for treating ... The effects of a systemic overdose will probably be similar to the effects of a nerve agent (they both act on the cholinergic ... Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary ... Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs). A recent ...
Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic GABAergic Histaminergic Melatonergic Monoaminergic ... Examples include glycine receptor agonists, glycine receptor antagonists, and glycine reuptake inhibitors. ...
link) Womer, DE; Shannon, HE (2000). "Reversal of pertussis toxin-induced thermal allodynia by muscarinic cholinergic agonists ... Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is a novel analgesic drug which acts as a mixed agonist-antagonist at ... May 1997). "Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053) a novel analgesic with mixed muscarinic receptor agonist and ... May 1997). "Butylthio[2.2.2] (NNC 11-1053/LY297802) an orally active muscarinic agonist analgesic". Journal of Pharmacology and ...
PHCCC selectively potentiated agonist-induced mGluR4 activity in cells expressing this receptor and did not itself act as an ... These drugs reduce the effect of acetylcholine in the brain by antagonizing cholinergic receptors. This helps restore the ... It is referred to as a dopamine receptor agonist. However, it does cause severe side effects when used on its own. ... Selegiline Rasagiline Dopamine receptor agonists. Directly increase the activity of the dopamine system. Apomorphine ...
Brain stimulation reward
... but there is counter-evidence suggesting some delta agonists might have weak ICSS facilitation properties. Cholinergic drugs ... Morphine, a MOR agonist, was one of the earliest studied drugs at the advent of ICSS and BSR. High potency MOR agonists like ... The effects of delta opioid receptor (DOR) agonists/antagonists on ICSS are less clear. One DOR agonist, SNC80, has been found ... GABAB receptor agonists and positive allosteric modulators have been found to result in ICSS depression and have been found to ...
... is a centrally acting anticholinesterase and indirect cholinergic agonist (parasympathomimetic). It was the first ...
Lieberman JA, Javitch JA, Moore H (August 2008). "Cholinergic agonists as novel treatments for schizophrenia: the promise of ... 1996). "PET study of the M1-agonists [11C]xanomeline and [11C]butylthio-TZTP in monkey and man". Dementia (Basel, Switzerland ... Jakubík J, Michal P, Machová E, Dolezal V (2008). "Importance and prospects for design of selective muscarinic agonists" (PDF ... Xanomeline (LY-246,708; Lumeron, Memcor) is a muscarinic acetylcholine receptor agonist with reasonable selectivity for the M1 ...
... is a partial agonist of the 5-HT6 receptor. It enhanced recognition memory and reversed the memory deficits of ... The mechanism of memory enhancement is due to a combined modulation of cholinergic and glutamatergic neurotransmission. E-6837 ... Kendall, I. (February 2011). "E-6801, a 5-HT6 receptor agonist, improves recognition memory by combined modulation of ... cholinergic and glutamatergic neurotransmission in the rat". Psychopharmacology. 213 (2-3): 413-30. doi:10.1007/s00213-010-1854 ...
Pretreatment with E1R enhanced the σ1R agonist PRE-084's stimulating effect and facilitated passive avoidance retention. It ... E1R enhances cognition and has efficacy against cholinergic dysfunction in mice without affecting locomotor activity. ...
Myosin binding protein C, cardiac
Hartzell HC, Titus L (Feb 1982). "Effects of cholinergic and adrenergic agonists on phosphorylation of a 165,000-dalton ...
Examples include excitatory amino acid receptor agonists, excitatory amino acid receptor antagonists, and excitatory amino acid ... Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic GABAergic GHBergic Glycinergic Histaminergic Melatonergic ...
Muscarinic acetylcholine receptor
Muscarinic agonist Muscarinic antagonist Nicotinic acetylcholine receptor Nicotinic agonist Nicotinic antagonist Eglen RM (July ... Very few parts of the sympathetic system use cholinergic receptors. In sweat glands the receptors are of the muscarinic type. ... Also, only when bound with an agonist, those G proteins normally sensitive to PTX also become susceptible to CTX. The various G ... Possible bronchospasm may result if stimulated by muscarinic agonists Location of M5 receptors is not well known. Like the M1 ...
... a cholinergic agonist, in the treatment of adults with attention deficit hyperactivity disorder". Am J Psychiatry. 156 (12): ... Potter A, Corwin J, Lang J, Piasecki M, Lenox R, Newhouse PA (March 1999). "Acute effects of the selective cholinergic channel ... It acts as an agonist at neural nicotinic acetylcholine receptors, subtype-selective binding with high affinity to the α4β2, α7 ... Wilens TE, Decker MW (October 2007). "Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity ...
Some different classes of GABAergic drugs include the following: GABA receptor agonists, GABA receptor antagonists, and GABA ... Adenosinergic Adrenergic Cannabinoidergic Cholinergic Dopaminergic Glycinergic Histaminergic Melatonergic Monoaminergic ...
"In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro". Psychopharmacology. ... Alvameline (Lu 25-109) is a M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of ... A quite different tack involves developing compounds that have cholinergic activity in their own right. The tetrazole ... yielding the muscarinic agonist alvameline (8). Milameline Sabcomeline Tazomeline Xanomeline Sánchez C, Arnt J, Didriksen M, ...
As all cholinergic fibers contain high concentrations of ACh and AChE at their terminals, inhibition of AChE can impair their ... This phenomenon is caused by the excess of agonists (ACh) within the synapse, ultimately leading to a down-regulation of ... Cholinergic nerves play an important role in the normal function of the central nervous, endrocrine, neuromuscular, ... When patients are resistant to atropine, the patients can be treated with low doses of anisodamine, a cholinergic and alpha-1 ...
Like the tropanes, it acts on cholinergic neurons, but with the opposite effect (it is an agonist as opposed to an antagonist ... They can reverse cholinergic poisoning, which can be caused by overexposure to organophosphate insecticides and chemical ...
The symptoms of nicotine poisoning are caused by excessive stimulation of nicotinic cholinergic neurons. Nicotine is an agonist ... Nicotine is specific for nicotinic cholinergic receptors only and has some, but not all of the symptoms of organophosphate ... excessive stimulation of all types of cholinergic neurons, and a wide range of symptoms. ...
Adenosine A1 receptor
Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... A1 receptors are implicated in sleep promotion by inhibiting wake-promoting cholinergic neurons in the basal forebrain. A1 ... cyclohexyladenosine Tecadenoson is an effective A1 adenosine agonist, as is selodenoson. 2‑Amino-3-(4′-chlorobenzoyl)-4- ...
A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys. Journal of Pharmacology and ... Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity disorder: focus on cognition. ... Central nicotinic receptor agonists ABT-418, ABT-089, and (−)-nicotine reduce distractibility in adult monkeys. ... ABT-089, a neuronal nicotinic receptor partial agonist, for the treatment of attention-deficit/hyperactivity disorder in adults ...
One specific drug candidate is BB14, which is a nerve growth factor-like peptide that acts as a TrkA agonist. BB14 was shown to ... For example, a few studies have used nerve growth factors to regain some cholinergic function in patients with Alzheimer's. ...
Injection of a cholinergic agonist (e.g. carbachol), into the pontine tegmentum produces a state of REM sleep in cats. PET ... Woolf, NJ; Butcher, LL (2011). "Cholinergic systems mediate action from movement to higher consciousness". Behavioural Brain ... The pontine tegmentum contains two predominately cholinergic nuclei, the pedunculopontine nucleus (PPN) and the laterodorsal ... the mesopontine cholinergic system comprising the pedunculopontine nucleus and the laterodorsal tegmental nucleus, and the ...
Direct-binding agonists can be further characterized as full agonists, partial agonists, inverse agonists. ... Activity of PT cholinergic neurons (REM-on cells) promotes REM sleep. During waking, REM-on cells are inhibited by a subset of ... An agonist of a neurotransmitter will thus initiate the same receptor response as the transmitter. In neurons, an agonist drug ... Such drugs are called receptor agonists. An example of a receptor agonist is Valium, a benzodiazepine that mimics effects of ...
Intestinal Motility Disorders Medication: Cholinergic Agonists, Prokinetic Agents, Opioid Reversal Agents, Antidiarrheals,...
Cholinergic Agonists. Class Summary. Excessive parasympathetic suppression appears to be involved in the genesis of intestinal ... Drugs used in the management of intestinal motility disorders include cholinergic agonists, prokinetic agents, opioid ... Tegaserod is a serotonin type 4 receptor partial agonist with no affinity for 5-HT3 receptors. It may trigger peristaltic ... Cholinergic agents may allow early resolution of pseudo-obstruction and obviate surgery. ...
Lambert-Eaton Myasthenic Syndrome (LEMS) Medication: Potassium Channel Blockers, Cholinergic Agonists, Immunosuppressants,...
Cholinergic Agonists. Class Summary. Cholinergic agonists produce symptomatic improvement in strength, autonomic symptoms, or ... resulting in ACh accumulation at synapses and increasing stimulation of cholinergic receptors at myoneural junction. ... of Lambert-Eaton myasthenic syndrome synaptic impairment by the combined use of a K+ channel blocker and a Ca2+ channel agonist ...
Cholinergic Agonists - Semantic Scholar
Any agent that is capable of activating cholinergic receptors (nicotinic and muscarinic) or of enhancing or prolonging the ... Cholinergic Agonists. Known as: Cholinergic Agonist, Agonists, Cholinergic, Acetylcholine Agonists (More). Any agent that is ... Cholinergic agonists inhibit HMGB1 release and improve survival in experimental sepsis. *Hong Wang, Hong Liao, +9 authors L. ... Cholinergic agonists attenuate renal ischemia-reperfusion injury in rats.. *Michael M Yeboah, Xiangying Xue, +4 authors ...
Evidence for presynaptic inhibition of the olfactory commissural pathway by cholinergic agonists and stimulation of the nucleus...
Evidence for presynaptic inhibition of the olfactory commissural pathway by cholinergic agonists and stimulation of the nucleus ... Evidence for presynaptic inhibition of the olfactory commissural pathway by cholinergic agonists and stimulation of the nucleus ... Evidence for presynaptic inhibition of the olfactory commissural pathway by cholinergic agonists and stimulation of the nucleus ... Evidence for presynaptic inhibition of the olfactory commissural pathway by cholinergic agonists and stimulation of the nucleus ...
Characterization of buccal motor programs elicited by a cholinergic agonist applied to the cerebral ganglion of Aplysia...
Characterization of buccal motor programs elicited by a cholinergic agonist applied to the cerebral ganglion of Aplysia ... Applying the non-hydrolyzable cholinergic agonist carbachol (CCh) to the cerebral ganglion of Aplysia elicits sustained, ...
Frontiers | Canonical and Novel Non-Canonical Cholinergic Agonists Inhibit ATP-Induced Release of Monocytic Interleukin-1β via...
In conclusion, we demonstrate that canonical nicotinic agonists and phosphocholine elicit metabotropic nAChR activity in ... Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that ... Furthermore, we identified phosphocholine and dipalmitoylphosphatidylcholine as novel nicotinic agonists that elicit ... function as nAChR agonists. In peripheral blood mononuclear cells from nAChR gene-deficient mice, we demonstrated that ...
REACTIVITY OF CHICK EMBRYO HEART TO CHOLINERGIC AGONISTS DURING ONTOGENESIS: DECLINE IN DESENSITIZATION AT THE ONSET OF...
... chick embryo atria underwent a change in reactivity to tetrodotoxin and to cholinergic agonists at the time of cholinergic ... REACTIVITY OF CHICK EMBRYO HEART TO CHOLINERGIC AGONISTS DURING ONTOGENESIS: DECLINE IN DESENSITIZATION AT THE ONSET OF ... REACTIVITY OF CHICK EMBRYO HEART TO CHOLINERGIC AGONISTS DURING ONTOGENESIS: DECLINE IN DESENSITIZATION AT THE ONSET OF ... REACTIVITY OF CHICK EMBRYO HEART TO CHOLINERGIC AGONISTS DURING ONTOGENESIS: DECLINE IN DESENSITIZATION AT THE ONSET OF ...
Pharmacological Characterization of SIB-1765F: A Novel Cholinergic Ion Channel Agonist | Journal of Pharmacology and...
Pharmacological Characterization of SIB-1765F: A Novel Cholinergic Ion Channel Agonist. Aida I. Sacaan, Richard T. Reid, Emily ... Pharmacological Characterization of SIB-1765F: A Novel Cholinergic Ion Channel Agonist. Aida I. Sacaan, Richard T. Reid, Emily ... Pharmacological Characterization of SIB-1765F: A Novel Cholinergic Ion Channel Agonist. Aida I. Sacaan, Richard T. Reid, Emily ... Pharmacological Characterization of SIB-1765F: A Novel Cholinergic Ion Channel Agonist Message Subject (Your Name) has ...
Cholinergic agonists and antagonists Flashcards by Leslie Rea | Brainscape
Study Cholinergic agonists and antagonists flashcards from Leslie Rea ... Cholinergic agonists and antagonists Flashcards Preview Pharm , Cholinergic agonists and antagonists , Flashcards ... 1. muscarine → muscarinic agonist. 2. Arecoline → muscarinic and nicotinic agonist. 3. Pilocarpine → mainly muscarinic agonist ... 1. What is the difference b/t a direct-acting and indirect-acting cholinergic agonist? ...
The Safety and Tolerance of Xanomeline Tartrate, an M1-Specific Cholinergic Agonist, in Patients with Alzheimer's Disease |...
... is a potent and selective M1 agonist that crosses the blood... ... an M1-Specific Cholinergic Agonist, in Patients with ... Cholinergic Agonist Healthy Elderly Subject Orthostatic Blood Pressure Moderate Nausea Moderate Diarrhea These keywords were ... an M1-Specific Cholinergic Agonist, in Patients with Alzheimers Disease. In: Hanin I., Yoshida M., Fisher A. (eds) Alzheimers ... Clinical trials of other cholinergic compounds have shown that the AD patient population frequently tolerates drugs quite ...
EP2062595A1 - Inhibition of inflammation using alpha 7 receptor-binding cholinergic agonists - Google Patents
The methods comprise treating the macrophage with a cholinergic agonist in an amount sufficient to decrease the amount of the ... Methods for determining whether a compound is a cholinergic agonist reactive with an α7 nicotinic receptor are also provided. ... These methods comprise determining whether the compound reduces the ability of a cholinergic agonist to inhibit the release of ... The methods comprise treating the patient with a cholinergic agonist in an amount sufficient to inhibit the inflammatory ...
Cholinergic agonist (2) | Article about cholinergic agonist (2) by The Free Dictionary
A contracting muscle that is resisted or... Explanation of cholinergic agonist (2) ... Find out information about cholinergic agonist (2). A chemical substance that can combine with a cell receptor and cause a ... Related to cholinergic agonist (2): Adrenergic agonist. agonist. [′ag·ə‚nist] (biochemistry) A chemical substance that can ... agonist. (redirected from cholinergic agonist (2)). Also found in: Dictionary, Thesaurus, Medical. ...
TREATMENT WITH CHOLINERGIC AGONISTS - Patent application
The cholinergic agonist compositions can be prepared with carriers that can protect the cholinergic agonist against rapid ... In certain embodiments, the cholinergic agonist is a muscarinic receptor agonist.  The term "muscarinic receptor agonist ... where the cholinergic agonist is administered as a suppository.  In various embodiments, the cholinergic agonist can be ... wherein the cholinergic agonist is administered intravaginally. 48. The method of claim 47, wherein the cholinergic agonist is ...
Karbachol - Analgesics, Non-Narcotic, Cardiotonic Agents, Cholinergic Agonists, Miotics, ATC:N07AB01, ATC...
Carbachol is a potent cholinergic (parasympathomimetic) agent which produces constriction of the iris and ciliary body ... Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs). ...
Muscarinic agonists We have already listed some non-selective muscarinic agonists. There are a few muscarinic agonists that are ... Other nicotinic agonists are lobeline (from the Lobelia plant), and dimethylphenylpiperazinium (DMPP), both of which favour ... ACh has similar agonist effects at both muscarinic and nicotinic receptors, but there are several other agents that favour ... The prototype agonist is muscarine, derived from the poisonous fly agaric, Amanita muscaria. ...
INHIBITION OF INFLAMMATORY CYTOKINE PRODUCTION BY CHOLINERGIC AGONISTS AND VAGUS NERVE STIMULATION - Patent application
... or no cholinergic agonist, which demonstrate that cholinergic agonists do not reduce LPS-stimulated TNF mRNA levels in ... 0040] As used herein, a cholinergic agonist is a compound that binds to cells expressing cholinergic receptor activity. The ... cholinergic agonist.  The neural-immune interaction described here, which we term the "cholinergic anti-inflammatory ... Cholinergic Agonists Inhibit Release of Proinflammatory Cytokines from Macrophages  1. Materials and Methods  Human ...
Complete Guide to Prescription & Nonprescription Drugs 2011 - H. Winter Griffith - Google Books
The revised and updated 2011 edition of the most accessible, comprehensive and affordable guide to prescription and nonprescription drugs. The classic guide to all major prescription and nonprescription drugs, featuring revised, up-to date FDA information and an A-Z list of medical conditions and their commonly used drugs for easy reference. It includes coverage of dosage and length of time before the drug takes effect, side effects, special precautions, interactions with other food and drugs, standards for use by different age groups, and much more. It also features a generic and brand name directory, a comprehensive glossary, and complete index by generic, brand, and class name.
Online Graduate Pharmacology Course | College of Nursing
Effects of Cholinergic and Adrenergic Agonists on Adenylate Cyclase Activity of Retinal Microvascular Pericytes in Culture - PDF
1, January 1992 Copyright Association for Research in Vision and Ophthalmology Effects of Cholinergic and Adrenergic Agonists ... The a 2 agonist clonidine decreased basal camp synthesis and reduced the effect of isoproterenol. The cholinergic agonist ... Effects of Cholinergic and Adrenergic Agonists on Adenylate Cyclase Activity of Retinal Microvascular Pericytes in Culture. ... forskolin with or without agonists, agonists in different concentration, or agonists with or without antagonists). On each day ...
The Pituitary - 4th Edition
Effect of Varenicline on Cognitive Function in Cigarette Smokers With Schizophrenia - Full Text View - ClinicalTrials.gov
Nicotinic Agonists. Cholinergic Agonists. Cholinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological ... Varenicline (VAR), an α4β2 nAChR partial agonist, approved for smoking cessation, mimics the effect of nicotine by stimulating ... It has been shown that neurocognitive deficits in schizophrenia improve by administration of nicotine, nicotinic agonists or ...
Tobacco Dependence Treatment for Asian Americans - Full Text View - ClinicalTrials.gov
Neurobiology of Nicotine and Non-nicotine Components of Tobacco Addiction - Full Text View - ClinicalTrials.gov
Clinical Management of the Elderly Patient in Pain: 1st Edition (Paperback) - Routledge
Cholinergic Agonists. * Gamma-Aminobutyric Acid Agonists. * Somatostatin. * Neuroleptics. * Aspirin and NSAIDs. * Conclusion. ...
Pilocarpine in Treating Patients With Dry Mouth Caused by Opioids - Full Text View - ClinicalTrials.gov
Salagen - FDA prescribing information, side effects and uses
cholinergic agonists pilocarpine, cevimeline, Evoxac. Xerostomia pilocarpine, glycerin topical, Biotene Mouthwash, NeutraSal, ... Cholinergic agonists may have dose-related central nervous system effects. This should be considered when treating patients ... Salagen® Tablets contain pilocarpine hydrochloride, a cholinergic agonist for oral use. Pilocarpine hydrochloride is a ... Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad spectrum of pharmacologic effects with predominant ...
RCSB PDB - 9PL Ligand Summary Page
Cholinergic Agonists. *Cholinergic Receptor Agonist. *Cytochrome P-450 CYP2A6 Inhibitors. *Cytochrome P-450 CYP2A6 Inhibitors ( ... agonist. Muscarinic acetylcholine receptor M4. MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGN.... unknown. partial agonist ... A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of ... agonist. Muscarinic acetylcholine receptor M2. MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKV.... unknown. ...
Cevimeline: Indications, Side Effects, Warnings - Drugs.com
Method of preparing polymeric adhesive compositions utilizing the mechanism of interaction between the polymer components -...
Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine<...
Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine. / Nowak, Thomas V.; Harrington, ... Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine. In: Gastroenterology. 1985 ; Vol. 88 ... Nowak, TV & Harrington, B 1985, Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine, ... Nowak TV, Harrington B. Effect of Cholinergic Agonists on Muscle From Rodent Proximal and Distal Small Intestine. ...
AntagonistsReceptorsPilocarpineCarbacholSelectiveReceptorNicotineAntagonistAdrenergicInhibitionCholineDrugsDopamineOxotremorineArecolineNeuronsNAChRSecretionScopolamineCevimelineSpecific agonistPharmacologyCorticalInhibitsAgentsNeurotransmissionNervous SystemAlzheimer'sRatsPreparationsAsthmaIndirectSynapsesBasal forebrainRegulationBethanecholExcitatoryGlucose
- Drugs used in the management of intestinal motility disorders include cholinergic agonists, prokinetic agents, opioid antagonists, antidiarrheals, and antibiotics. (medscape.com)
- Materials and Methods Agonists and Antagonists Prazosin was obtained from Pfizer (Brooklyn, NY). (healthdocbox.com)
- Muscarinic Agonists and Antagonists - Some Therapeutic Applications. (routledge.com)
- This has lead to a number of significant advances including 5HT 3 antagonists for the treatment of functional diarrhoea, 5HT 4 agonists for the treatment of constipation and 5HT 1 agonists for the treatment of impaired fundal relaxation. (wiley.com)
- As more specific agonists and antagonists have become available more discriminating studies have become possible to define these many separate and sometimes conflicting responses. (wiley.com)
- Adenosine receptors: development of selective agonists and antagonists. (biomedsearch.com)
- General anaesthetics are mainly GABA agonists but some (such as ketamine) are glutamate antagonists. (bio.net)
- Tegaserod is a serotonin type 4 receptor partial agonist with no affinity for 5-HT3 receptors. (medscape.com)
- Pyridostigmine blocks ACh hydrolysis by cholinesterase, resulting in ACh accumulation at synapses and increasing stimulation of cholinergic receptors at myoneural junction. (medscape.com)
- Any agent that is capable of activating cholinergic receptors (nicotinic and muscarinic) or of enhancing or prolonging the actions of acetylcholine. (semanticscholar.org)
- Nicotine, the prototypical agonist for neuronal nicotinic acetylcholine receptors (NAChR), nonselectively activates NAChR limiting its use in elucidating the function of NAChR subtypes. (aspetjournals.org)
- Recently, we discovered a cholinergic mechanism that inhibits the adenosine triphosphate (ATP)-dependent release of interleukin-1β (IL-1β) by human monocytes via nicotinic acetylcholine receptors (nAChRs) composed of α7, α9 and/or α10 subunits. (frontiersin.org)
- Note that the effects of cholinergic agents are complex, not only because of the existence of nicotinic and muscarinic receptors (and subclasses of these) but also because of the presynaptic and postsynaptic locations of such receptors. (anaesthetist.com)
- Epibatidine (from the Dendrobatid poison dart frog Epipedobates tricolor ) is a potent agonist at nicotinic receptors. (anaesthetist.com)
- Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs). (pharmacycode.com)
- These results suggest that pericytes have functional adrenergic and cholinergic receptors, and they might respond to autonomic vasoactive substances present in vivo. (healthdocbox.com)
- Other possible pharmacological strategies include increasing acetylcholine release with 5-HT 4 agonists or directly stimulating cholinergic receptors with muscarinic and nicotinic agonists. (nih.gov)
- We explored the possibility that APP processing is regulated by activation of endogenous cell-surface neurotransmitter receptors by stimulating C6, PC12 and neuroblastoma cells with the cholinergic agonist carbachol. (elsevier.com)
- These results suggest that the decrease in intracellular APP seen after stimulation by carbachol has some specificity and that APP processing may be regulated by stimulation of cholinergic receptors on the surface of cells. (elsevier.com)
- Here, we describe a role for central muscarinic acetylcholine receptors in the activation of the cholinergic antiinflammatory pathway. (pnas.org)
- Blockade of peripheral muscarinic receptors did not abolish antiinflammatory signaling through the vagus nerve, indicating that peripheral muscarinic receptors on immune cells are not required for the cytokine-regulating activities of the cholinergic antiinflammatory pathway. (pnas.org)
- The role of central muscarinic receptors in activating the cholinergic antiinflammatory pathway is of interest for the use of centrally acting muscarinic cholinergic enhancers as antiinflammatory agents. (pnas.org)
- Although the vagus nerve is a "classical" cholinergic regulator of visceral functions in which peripheral muscarinic acetylcholine receptors have a major mediating role, the vagus-nerve cytokine-inhibiting activity (which is termed "the cholinergic antiinflammatory pathway") requires signaling through nicotinic α 7 subunit-containing receptors ( 4 , 5 ). (pnas.org)
- In contrast, peripheral muscarinic receptors do not have a major role in mediating the inflammatory response to endotoxin and its inhibition by the cholinergic antiinflammatory pathway. (pnas.org)
- To study the role of central muscarinic receptors in the inhibition of serum TNF, we administered intracerebroventricularly (i.c.v.) the prototype muscarinic receptor agonist muscarine (0.5-500 ng/kg) before endotoxin exposure. (pnas.org)
- Muscarine dose-dependently inhibited serum TNF ( Fig. 1 A ). Postsynaptically located M1 subtype muscarinic receptors have an important role in the processing of cholinergic neurotransmission in the brain ( 11 , 12 ). (pnas.org)
- Nicotine acts as an agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist. (wikipedia.org)
- In Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. (wikipedia.org)
- The targets for muscarinic agonists include the following receptors: Muscarine Muscarinic acetylcholine receptor Muscarinic antagonist Nicotinic acetylcholine receptor Nicotinic agonist Nicotinic antagonist Fisher A, Brandeis R, Bar-Ner RH, Kliger-Spatz M, Natan N, Sonego H, Marcovitch I, Pittel Z. AF150(S) and AF267B: M1 muscarinic agonists as innovative therapies for Alzheimer's disease. (wikipedia.org)
-  Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. (wikipedia.org)
- they produce their effects by binding to and activating cholinergic receptors. (wikipedia.org)
- Head skin stimulation activates a cholinergic pathway which then opens G protein-coupled inward-rectifying potassium channels (GIRKs) via postsynaptic M muscarinic receptors to inhibit brainstem neurons critical for the initiation and maintenance of swimming for up to minutes and can explain many features commonly observed immediately after concussion. (bireme.br)
- Partial agonist and weak antagonist at mu receptors. (brainscape.com)
- A partial agonist produces less than the maximum effect even if given in a concentration sufficient to bind with all available receptors. (thefreedictionary.com)
- It is an agonist at both muscarinic and nicotinic acetylcholine receptors. (curehunter.com)
- Since the levamisole-receptor mutants responded to other cholinergic drugs, other acetylcholine receptors are likely to function in parallel with the levamisole-sensitive receptors to mediate cholinergic neurotransmission in the egg-laying circuitry. (genetics.org)
- Pilocarpine is a tertiary amine that is stable to hydrolysis by acetylcholinesterase and acts as a partial muscarinic agonist. (brainscape.com)
- Methods of treating disorders with cholinergic agonists for example, muscarinic receptor agonists such as pilocarpine and cevimeline are provided. (patentsencyclopedia.com)
- 50. The method of claim 49, wherein the muscarinic receptor agonist is pilocarpine or a pharmaceutically acceptable salt thereof. (patentsencyclopedia.com)
- Salagen ® Tablets contain pilocarpine hydrochloride, a cholinergic agonist for oral use. (drugs.com)
- Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad spectrum of pharmacologic effects with predominant muscarinic action. (drugs.com)
- The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. (drugs.com)
- In the form of pilocarpine, muscarinic receptor agonists have been used medically for a short time. (wikipedia.org)
- Pilocarpine is a drug that acts as a muscarinic receptor agonist that is used to treat glaucoma. (wikipedia.org)
- Pilocarpine is in a class of medications called cholinergic agonists. (medlineplus.gov)
- Pilocarpine, a cholinergic agonist, significantly reduced the high levels of serum prolactin in estrogen-primed male rats and in female rats on the late afternoon of proestrus. (semanticscholar.org)
- Applying the non-hydrolyzable cholinergic agonist carbachol (CCh) to the cerebral ganglion of Aplysia elicits sustained, regular bursts of activity in the buccal ganglia resembling those seen during biting. (nih.gov)
- Carbachol is a potent cholinergic (parasympathomimetic) agent which produces constriction of the iris and ciliary body resulting in reduction in intraocular pressure. (pharmacycode.com)
- Lahiri, DK , Nall, C & Farlow, MR 1992, ' The cholinergic agonist carbachol reduces intracellular β-amyloid precursor protein in PC 12 and C6 cells ', Biochemistry International , vol. 28, no. 5, pp. 853-860. (elsevier.com)
- This propulsive effect of the extract, similar to that of carbachol, was blocked in atropine-pretreated mice, a standard cholinergic antagonist. (springer.com)
- Among nonphotic stimulants, a classic cholinergic agonist, carbachol, is known to have a strong and unique phase-resetting effect on the circadian clock: Intracerebroventricular carbachol treatment causes phase delays during the subjective early night and phase advances in the subjective late night, but the effects of this drug on the suprachiasmatic nucleus (SCN) in vivo and in vitro are still controversial. (bireme.br)
- Xanomeline tartrate [3-(4-hexyloxy-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-l-methylpyridine tartrate], also known as LY246708 tartrate, is a potent and selective M1 agonist that crosses the blood brain barrier in animals and is orally bioavailable (Eli Lilly, unpublished data). (springer.com)
- Our results indicate that central cholinergic activation by selective muscarinic receptor ligands significantly inhibits systemic TNF in endotoxemic rats and activates the efferent vagus-nerve activity. (pnas.org)
- Convergent findings from neuroimaging and behavioral studies in both animals and humans suggest that the cholinergic system might also be critically implicated in selective attention by modulating cortical function via widespread projections from the basal forebrain. (frontiersin.org)
- Numerous findings in rodents and primates point to a critical role of cholinergic inputs to cortical areas, which are conveyed by the basal forebrain cholinergic nuclei through widespread projections and act to enhance selective attention. (frontiersin.org)
- M3 agonist which is more selective, potent in action at the salivary and lacrimal glands than others. (flashcardmachine.com)
- A selective beta-1-adrenergic partial agonist. (molecularstation.com)
- The decline in desensitization may be due to developmental changes in the atropine-sensitive cholinergic receptor and/or in the potassium conductance activatd by the drug-receptor interaction. (aspetjournals.org)
- In addition, intra-vaginal administration of cholinergic agonists such as muscarinic receptor agonists to patients suffering from interstitial cystitis, vaginal dryness, and sexual dysfunction associated with vaginal dryness is also provided. (patentsencyclopedia.com)
- 48. The method of claim 47, wherein the cholinergic agonist is a muscarinic receptor agonist. (patentsencyclopedia.com)
- Central muscarinic cholinergic activation by muscarine, the M1 receptor agonist McN-A-343, and the M2 receptor antagonist methoctramine inhibited serum TNF levels significantly during endotoxemia. (pnas.org)
- These findings identify a pivotal role for central muscarinic cholinergic activation in the inhibition of the systemic inflammatory response during endotoxemia and indicate that the cholinergic antiinflammatory pathway represents a peripheral muscarinic-receptor-independent cholinergic function of the vagus nerve. (pnas.org)
- A muscarinic receptor agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. (wikipedia.org)
- Muscarine is a nonselective agonist of the muscarinic acetylcholine receptor . (wikipedia.org)
- There is evidence that genetic variations in the M3 receptor are associated with early-onset type 2 diabetes and the acute insulin response in Pima Indians ( 17 ), but few studies have investigated cholinergic mechanisms in human islets ( 16 , 18 - 20 ). (diabetesjournals.org)
- It may be an agonist or partial agonist for a particular receptor, promoting a receptor-mediated biological response, often by competing with another substance (usually the natural or native substance) at the same receptor. (thefreedictionary.com)
- Name 2 natural alkaloids that are choinergic agonists and the receptor they target. (flashcardmachine.com)
- Abstract -Moxonidine is an I 1 -imidazoline receptor agonist that reduces blood pressure in hypertensives. (ahajournals.org)
- Agonists such as nicotine are mainly toxicological curiosities, rather than clinically useful drugs. (anaesthetist.com)
- It has been shown that neurocognitive deficits in schizophrenia improve by administration of nicotine, nicotinic agonists or cigarette smoking. (clinicaltrials.gov)
- Varenicline (VAR), an α4β2 nAChR partial agonist, approved for smoking cessation, mimics the effect of nicotine by stimulating nAChRs, and releasing sufficient dopamine in order to reduce craving and withdrawal effects. (clinicaltrials.gov)
- The muscarinic cholinergic antagonist atropine significantly blunted the ACTH response to arecoline. (euc.ac.cy)
- A spasmolytic effect was also observed in other gut preparations either as noncompetitive inhibition of agonist dose-response curves, inhibition of high K + (80 mM)-induced contractions, or displacement of Ca 2+ dose-response curves to the right, indicating a calcium antagonist effect. (springer.com)
- An antagonist is a molecule that interferes with or prevents the action of the agonist. (thefreedictionary.com)
- Because it is a partial agonist (DRUG PARTIAL AGONISM) it acts like an agonist when sympathetic activity is low and as an antagonist when sympathetic activity is high. (molecularstation.com)
- Evidence suggested that desensitization, most prominently observed with carbamylcholine, restricted the duration of cholinergic inhibition of the pacemaker on the 6th incubation day. (aspetjournals.org)
- At cholinergic synapses there is also a presynaptic transporter - the difference is that ACh is first hydrolysed back to acetate and choline, and then choline is avidly taken up. (anaesthetist.com)
- 2-4 Subsequent discoveries of reduced choline uptake, 5 ACh release 6 and loss of cholinergic perikarya from the nucleus basalis of Meynert 7 confirmed a substantial presynaptic cholinergic deficit. (bmj.com)
- Using choline as a nAChR partially subtype-specific agonist, we found that the majority of DS GCs demonstrated responses to choline while under synaptic blockade. (cambridge.org)
- Because choline is a partial agonist for α3β4 nAChRs (Alkondon et al. (cambridge.org)
- Clinical trials of other cholinergic compounds have shown that the AD patient population frequently tolerates drugs quite differently from healthy volunteers (Cutler et al. (springer.com)
- Many drugs are agonists having an effect similar or identical to natural body agonists. (thefreedictionary.com)
- What are the classes and subclasses of Cholinergic drugs? (flashcardmachine.com)
- This article examines the existing scientific applicability of the original cholinergic hypothesis of Alzheimer's disease by describing the biochemical and histopathological changes of neurotransmitter markers that occur in the brains of patients with Alzheimer's disease both at postmortem and neurosurgical cerebral biopsy and the behavioural consequences of cholinomimetic drugs and cholinergic lesions. (bmj.com)
- We tested whether the cerebral blood flow (CBF) response to the cholinergic agonist oxotremorine (OXO) is affected by the choice of anesthetics in dogs. (elsevier.com)
- The cholinergic agonist oxotremorine did not modify the basal activity of adenylate cyclase but was able to decrease by almost 50% the forskolin-induced increase of camp. (healthdocbox.com)
- Subcellular distribution of m4R immunoreactivity in striatal cholinergic neurons of control rats ( A ) or rats treated with oxotremorine ( B ) using pre-embedding immunogold method with silver intensification. (jneurosci.org)
- To examine the site on the HPA axis that is stimulated by cholinergic agents, we evaluated the in vivo and in vitro effects of the muscarinic cholinergic agonist arecoline in intact and pituitary stalk-transected rats as well as on isolated rat hypothalami, dispersed anterior pituicytes, and adrenocortical cells in culture. (euc.ac.cy)
- These data suggest that the muscarinic cholinergic agonist arecoline stimulates the HPA axis in the rat and that this effect is mediated mainly by the release of endogenous CRH. (euc.ac.cy)
- Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. (frontiersin.org)
- The purpose of this study is to determine the composition of nAChRs necessary for nicotinic signaling in monocytic cells and to test the hypothesis that common metabolites of phosphatidylcholines, lysophosphatidylcholine (LPC) and glycerophosphocholine (G-PC), function as nAChR agonists. (frontiersin.org)
- In conclusion, we demonstrate that canonical nicotinic agonists and PC elicit metabotropic nAChR activity in monocytes via interaction of nAChR subunits α7, α9 and α10. (frontiersin.org)
- Because somatostatin is a strong inhibitor of insulin secretion, we hypothesized that cholinergic input to the δ-cell indirectly regulates β-cell function. (diabetesjournals.org)
- Endogenous cholinergic signaling therefore provides direct stimulatory and indirect inhibitory input to β-cells to regulate insulin secretion from the human islet. (diabetesjournals.org)
- whereas cholinergic blockade (e.g., by scopolamine) can severely interfere with attention and increase distraction (see e.g. (frontiersin.org)
- Cevimeline (AF102B) (Evoxac ) is a muscarinic agonist that is an Food and Drug Administration (FDA)-approved drug and used for the management of dry mouth in Sjögren's syndrome. (wikipedia.org)
- What is a new M3 specific agonist? (flashcardmachine.com)
- Pharmacology Agonist medication. (thefreedictionary.com)
- Cortical cholinergic denervation resulting from degeneration of the nucleus basalis of Meynert (NBM) is a primary contributor to cognitive impairment and neuropsychiatric symptoms in the Lewy body diseases Parkinson's disease (PD), Parkinson's disease dementia (PDD), and dementia with Lewy bodies (DLB). (nih.gov)
- The authors review the current landscape of pharmacological and surgical therapies for mitigating the cortical cholinergic deficiency in PD, PDD, and DLB. (nih.gov)
- Targeting the basal forebrain with either deep brain stimulation (DBS)- or cell-based therapies is another strategy to mitigate cortical cholinergic deficiency. (nih.gov)
- Cholinergic Modulation of Cortical activity. (routledge.com)
- Here we asked whether deficits in spatial attention associated with neglect could partly result from a cholinergic deafferentation of cortical areas subserving attentional functions, and whether such disturbances could be alleviated by pro-cholinergic therapy. (frontiersin.org)
- Activation of this "cholinergic antiinflammatory pathway" inhibits the production of TNF and other cytokines and protects animals from the inflammatory damage caused by endotoxemia and severe sepsis. (pnas.org)
- Cholinergic agents may allow early resolution of pseudo-obstruction and obviate surgery. (medscape.com)
- PMID 12212772 Fisher A. M1 muscarinic agonists: Their potential in treatment and as disease-modifying agents in Alzheimer's disease Drug Dev. (wikipedia.org)
- Treatment of Disorders Characterized by Reversible Airway Obstruction in Childhood: are Anti-cholinergic Agents the Answer? (eurekaselect.com)
- Such studies have resulted in the discovery of an association between a decline in learning and memory, and a deficit in excitatory amino acid (EAA) neurotransmission, together with important roles for the cholinergic system in attentional processing and as a modulator of EAA neurotransmission. (bmj.com)
- however, the genetic and molecular basis for cholinergic neurotransmission in the egg-laying circuitry is not well understood. (genetics.org)
- Muscarine mimics the function of the natural neurotransmitter acetylcholine in the muscarinic part of the cholinergic nervous system, despite the less flexible structure due to the five-membered ring in the molecular skeleton. (wikipedia.org)
- Cholinergic agonist medications stimulate the involuntary nervous system. (sharecare.com)
- More specifically, it explores neurochemical interactions by focusing on the relationship between cholinergic and monoaminergic mechanisms in the central nervous system. (elsevier.com)
- Organized into six sections comprised of 18 chapters, this volume begins with an overview of various models of cholinergic-monoaminergic and other chemical interactions, based in part on interactive processes that are believed to operate in the peripheral nervous system. (elsevier.com)
- A cholinergic drug, C 7 H 16 N 2 O 2 , that is used in the form of its chloride to treat urinary retention by stimulating the parasympathetic nervous system. (thefreedictionary.com)
- Cutler N.R., Sramek J.J., Seifert R.D., Conrad J.J., Wardle T.S. (1995) The Safety and Tolerance of Xanomeline Tartrate, an M1-Specific Cholinergic Agonist, in Patients with Alzheimer's Disease. (springer.com)
- The cholinergic system has been recognized as playing an important role not only in several forms of dementia besides Alzheimer's Disease, but also in other CNS degenerative and psychiatric disorders. (routledge.com)
- Cholinergic Synaptic Terminations in the Cerebral Cortex, Trophic Factor Dependency and Vulnerability to Aging and Alzheimer's Pathology. (routledge.com)
- Accordingly, although there is presently no "cure" for Alzheimer's disease, a large number of potential therapeutic interventions have emerged that are designed to correct loss of presynaptic cholinergic function. (bmj.com)
- Cholinergic agonists attenuate renal ischemia-reperfusion injury in rats. (semanticscholar.org)
- Abnormal central cholinergic activity has been reported to be responsible in part for the pathogenesis of high blood pressure in spontaneously hypertensive rats (SHR). (ahajournals.org)
- Nicotinic agonists produced augmented pressor, heart rate, and irritation responses in SHRLJ compared with normotensive rats. (ahajournals.org)
- Cardioinhibition persisted throughout the 5-minute exposure to cholinergic agonists in sinoatrial preparations from the 12th and l8th incubation days whereas automaticity recovered completely within 1 to 2 minutes in preparations from the 6th incubation day. (aspetjournals.org)
- These data indicate that Zo.Cr contains a cholinergic, spasmogenic component evident in stomach fundus preparations which provides a sound mechanistic insight for the prokinetic action of ginger. (springer.com)
- If you have asthma, cholinergic agonists may not be good options for you. (sharecare.com)
- The Contribution of the Basal Forebrain Cholinergic System to Neuronal Plasticity. (routledge.com)
- Muscarinic cholinergic regulation of cardiac myocyte ICa-L is absent in mice with targeted disruption of endothelial nitric oxide synthase. (semanticscholar.org)
- Bethanechol is a cholinergic agent used to treat urinary retention related to bladder atony. (thefreedictionary.com)
- Consider a trial of a cholinergic agonist, such as bethanechol , in patients with urinary retention. (thefreedictionary.com)
- The second approach is to attempt to correct the lysosomal defect by a cholinergic agonist, bethanechol chloride. (thefreedictionary.com)
- Cholinergic agonists prime the beta-cell to glucose stimulation. (semanticscholar.org)