ReceptorsAntagonistMuscarinic cholinergicVarious agonistsContractile response to carbacholPhosphatidylinositol hydrolysisCholinergic agonistsInhibitoryAcetylcholine receptorBethanecholHydrolysisGastric acid secretionInduceSelectiveReceptorPilocarpineHippocampal slicesTreatment of glaucomaOxotremorineIntraocularAtropineInhibitContractionPartialConcentrationsCell MembraneMAChRGlaucomaBladderNicotinePotencyInhibitionAsthmaLipidCurrentsAccumulationEffectsSignificantlyAffinityCompoundResponseMembranesDrugsExperimentsConcentrationCellsInteractResponses
Receptors14
- Carbachol, also known as carbamylcholine and sold under the brand name Miostat among others, is a cholinomimetic drug that binds and activates acetylcholine receptors. (wikipedia.org)
- Carbachol is a parasympathomimetic that stimulates both muscarinic and nicotinic receptors. (wikipedia.org)
- Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs). (wikipedia.org)
- In phosphatidylinositol hydrolysis assays, muscarinic agonists showed greater potency at the HM 1 (S388Y) and HM 1 (S388Y, T389P) mutants compared with the wild-type and HM 1 (T389P) receptors. (aspetjournals.org)
- Although nicotine is an agonist of ionotropic acetylcholine receptors, we found that nicotine-induced polyspermy was neither mimicked by acetylcholine and carbachol nor inhibited by specific antagonists of nicotinic acetylcholine receptors. (mdpi.com)
- The muscarinic receptor antagonists atropine, scopolamine and PZ inhibited the binding of [3H]QNB and [3H]PZ to solubilized receptors with Hill slopes of 1, as did the muscarinic receptor agonist oxotremorine. (unboundmedicine.com)
- The S-S reducing agent, dithiothreitol (DTT) altered the properties of nicotinic receptors in rat superior cervical ganglia such that (i) carbachol became less active as a depolarizing agent and (ii) bromo- acetylcholine produced an irreversible depolarization. (ox.ac.uk)
- It is concluded that ganglionic nicotinic receptors might be quite similar to those for monoquaternary agonists in leech dorsal muscle. (ox.ac.uk)
- These data suggest that ergotamine is in principle an agonist at human 5-HT4-serotonin receptors as well at human H2-histamine receptors. (bvsalud.org)
- Ergotamine acts as an agonist on H2-histamine receptors in the human atrium. (bvsalud.org)
- 5. Block of carbachol activation of muscarinic receptors with atropine (10 μM) abolished the elevation of [Ca 2+ ](i) by the opioids. (edu.au)
- Both classical and atypical agonists activate hM1 receptors by the same molecular switch that involves D71 in the second transmembrane helix. (cas.cz)
- The improvement of therapeutic approaches using specific mAChR modulators is further impeded by a lack of established and validated protocol to screen efficacy of different mAChR agonist/antagonist at native receptors in neocortical slices. (biomedcentral.com)
- The maximum effect of the drug may be produced even if not all receptors are bound in the presence of which of the following: A. Full agonist B. Partial agonist C. Spare receptors D. Inert binding site E. Effector 7. (kupdf.net)
Antagonist2
- The carbachol-induced response is sensitive to atropine, a muscarinic-cholinergic antagonist, but not mecamylamine a nicotinic-cholinergic antagonist, while that of norepinephrine is blocked by the α l adrenoreceptor antagonist prazosin, but not the specific α 2 antagonist Rx 781094. (elsevierpure.com)
- The nicotinic receptor antagonist, mecamylamine (10 μM), did not affect the elevations of [Ca 2+ ](i) caused by opioids in the presence of carbachol. (edu.au)
Muscarinic cholinergic2
- The high K + -Krebs solution and the muscarinic cholinergic agonist, carbachol evoked a sustained contraction in normal mice bladder strips. (basicmedicalkey.com)
- The maximum contractile response to the muscarinic cholinergic agonist carbachol is determined as a percent of the maximum contraction to the response induced by the high-K solution. (basicmedicalkey.com)
Various agonists2
- Slices were preincubated with [ 3 H]-myo-inositol and the accumulation of [ 3 H]-myo-inositol-1-phosphate induced by various agonists was determined in the presence of 10 mM lithium. (elsevierpure.com)
- We investigated the effects of the cholinergic agonist carbachol (CCh) and various agonists and antagonists on neuronal activity in rat neocortical slices using intracellular (sharp microelectrode) and field potential recordings. (biomedcentral.com)
Contractile response to carbachol2
- In order to elucidate the mechanism of functional changes in aged rat urinary bladder, we studied the influence of senescence on, 1) the α-adrenergic contractile response to phenylephrine in the urinary bladder body and trigone, 2) the muscarinic contractile response to carbachol in the body and trigone. (scirp.org)
- Maximum contractile response to carbachol. (basicmedicalkey.com)
Phosphatidylinositol hydrolysis2
- These data suggest that phorbol ester receptor-mediated events may be negatively coupled to agonist-induced phosphatidylinositol hydrolysis. (wustl.edu)
- The stimulation of phosphatidylinositol hydrolysis by various neurotransmitter agonists was investigated in rat hippocampal slices using a rapid and sensitive radioisotopic method. (elsevierpure.com)
Cholinergic agonists1
- It was previously demonstrated that high concentrations of cholinergic agonists such as acetylcholine (ACh), carbamylcholine (CCh), suberyldicholine (SubCh) and spin-labelled acetylcholine (SL-ACh) displaced quinacrine from its high-affinity binding site located at the lipid-protein interface of the nicotinic acetylcholine receptor (AChR) (Arias, H. R. and Johnson, D. A. (1995) Biochemistry, 34, 1589-1595). (okstate.edu)
Inhibitory3
- Greater inhibitory effects were seen with stimulants such as carbachol and cyclopiazonic acid (CPA) rather than with forskolin or protein kinase A activators. (mcmaster.ca)
- LSD-induced attenuations of CVEP and aubcortical VEP suggest this agent may act as an agonist at low doses on an inhibitory serotonergic system. (erowid.org)
- The inhibitory conductances were unaltered by xanomeline (M 1 /M 4 mAChRs agonist), yet the CCh-induced depression was antagonized by AF-DX 116. (biomedcentral.com)
Acetylcholine receptor1
- They show that treating cultured mouse neurons expressing human APP with the acetylcholine receptor agonist carbachol increased the production of α-secretase cleavage products, but no such effect occurred in cells from M1 knockout mice. (alzforum.org)
Bethanechol1
- Cholinergic agonist like carbachol, bethanechol and pilocarpine bind to GPCR and produce their pharmacological actions. (egpat.com)
Hydrolysis2
- No difference was noted in the ability of carbachol to stimulate phosphoinositide hydrolysis in the two species. (cdc.gov)
- The hydrolysis of phosphatidylinositol in hippocampal slices is induced by carbachol, serotonin, norepinephrine and phenylephrine. (elsevierpure.com)
Gastric acid secretion1
- Peptic ulcer: Choline esters (muscarinic agonists), by increasing gastric acid secretion, may exacerbate ulcer symptoms. (pharmacology2000.com)
Induce3
- In the cat and rat, carbachol is well known for its ability to induce rapid eye movement (REM) sleep when microinjected into the pontine reticular formation. (wikipedia.org)
- In rat hippocampal slices, carbachol and norepinephrine induce an accumulation of [ 3 H]-inositol-1-phosphate which is markedly amplified in the presence of lithium. (wustl.edu)
- Hyperthyroidism: Choline esters (muscarinic agonists) can induce atrial fibrillation in hyperthyroid patients. (pharmacology2000.com)
Selective5
- Their work, published in the March 24 Journal of Neuroscience, offers support for the ongoing development of M1-selective agonists as modulators of amyloid load. (alzforum.org)
- We compared the effects of these mutations on the action of two atypical M1 functionally preferring agonists (N-desmethylclozapine and xanomeline) and two classical non-selective orthosteric agonists (carbachol and oxotremorine). (cas.cz)
- However, the similarity in ligand-binding sites between mAChR subtypes, the paucity of selective agonists/antagonists as well as the expression of different subtypes of mAChRs in a given area constitute major obstacles to delineate cellular effects of a given subtype [ 1 ]. (biomedcentral.com)
- Epinephrine and carbachol did not affect the Ca2+ channel current reduced by the dihydropyridine, PN 200-110 (1 microM), suggesting a selective inhibition of dihydropyridine-sensitive Ca2+ channels. (mdc-berlin.de)
- In contrast, a selective α-adrenergic agonist phenylephrine, elicited greater contractions both in the aged body and trigone than those in young rats. (scirp.org)
Receptor11
- Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary insufficiency, gastroduodenal ulcers, and incontinence. (wikipedia.org)
- A human M 1 (HM 1 ) mutant receptor, HM 1 (S388Y, T389P), displayed significantly enhanced agonist potency, binding affinity, and G protein coupling. (aspetjournals.org)
- The muscarinic receptor agonist carbachol competed for [3H]QNB and [3H]PZ binding with a Hill slope of less than 1 in cerebral cortex, but not in cerebellum. (unboundmedicine.com)
- GTP did not alter the interactions of carbachol or oxotremorine with the solubilized receptor. (unboundmedicine.com)
- Together, these data suggest that muscarinic receptor sites solubilized from rat brain retain their abilities to interact selectively with muscarinic receptor agonists and antagonists. (unboundmedicine.com)
- Expressing M1 receptor in knockout cells restored carbachol-induced α-secretase processing. (alzforum.org)
- Selectivity is important on both counts: Non-specific muscarinic receptor agonists can produce side effects due to peripheral cholinergic effects including gastrointestinal disturbances, changes in blood pressure, and excessive sweating. (alzforum.org)
- In addition, Davis and coworkers show that treating neurons from M1 knockout mice with carbachol increased Aβ production, probably via stimulation of other non-M1 muscarinic receptor subtypes. (alzforum.org)
- An examination was also undertaken of the muscarinic receptor function in rat and rabbit brain by measuring the accumulation of inositol phosphates in cerebral cortex slices following stimulation by the cholinergic agonist carbachol. (cdc.gov)
- Our results suggest that the measurement of agonist-induced [ 3 H]-myo-inositol-1-phosphate accumulation, in the presence of lithium, represents a sensitive method for studying a number of receptor-mediated events in brain. (elsevierpure.com)
- Mutation of the residues involved in receptor activation (D71) and coupling to G-proteins (R123) completely abolished the functional responses to both classical and atypical agonists. (cas.cz)
Pilocarpine1
- Carbachol and pilocarpine are two of the drugs indicated for treatment of glaucoma. (egpat.com)
Hippocampal slices1
- The tumor-promoting agents phorbol 12, 13-dibutyrate (PDB) and 4β phorbol, 12β-myristate, 13 α-acetate (PMA) have no effect on [ 3 H] inositol-1-phophate accumulation alone, but when preincubated with hippocampal slices significantly inhibit the accumulation of [ 3 H]-inositol-1-phosphate induced by carbachol and norepinephrine. (wustl.edu)
Treatment of glaucoma2
- Carbachol is primarily used in the treatment of glaucoma, but it is also used during ophthalmic surgery. (wikipedia.org)
- Carbachol may be used also in treatment of glaucoma. (pharmacology2000.com)
Oxotremorine1
- Mutation of D105 decreased the potency of the atypical agonist xanomeline more than that of the classical agonists carbachol and oxotremorine. (cas.cz)
Intraocular1
- Carbachol is not easily metabolized by cholinesterase, it has a 2 to 5 minute onset of action and its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration. (wikipedia.org)
Atropine1
- The effect of carbachol was abolished by atropine. (mdc-berlin.de)
Inhibit1
- To further assess the differences in agonist accessibility to the quinacrine binding site, we calculated the agonist concentration in the lipid membrane (C M ) at an external agonist concentration high enough to inhibit 50% of quinacrine binding (IC 50 ), which in turn was obtained by agonist back titration of AChR-bound quinacrine. (okstate.edu)
Contraction2
- Carbachol-induced contraction in aged rat bladder was identical to that obtained in young rat. (scirp.org)
- There were no significant differences of the percentage of the carbachol-induced maximum contraction for the high K + -Krebs solution-induced ones between both the groups. (basicmedicalkey.com)
Partial2
- However, higher doses of LSD were incapable of reversing cinanserin blockade, suggesting LSD also be a partial agonist. (erowid.org)
- Phenylephrine, another α 1 adrenoreceptor agonist produced a partial or submaximal response when compared to norepinephrine. (elsevierpure.com)
Concentrations3
- Tubulin, at nanomolar concentrations, transactivated Gαq by the direct transfer of a GTP analog and potentiated carbachol-activated PLCβ 1 . (jneurosci.org)
- In contrast, the weak tumor promoting agents 4-O-methylphorbol 12 myristate 13 acetate (MPMA) and phorbol 13,20-diacetate (P 13,20 DA) only slightly attenuate the agonist-induced response at concentrations ≤100μM, whereas 4α-phorbol (4α-PHR), a biologically inactive phorbol, has no effect. (wustl.edu)
- initial experiments established that high agonist concentrations do not affect either transmembrane proton concentration equilibria (pH) of AChR membrane suspension or AChR-bound quinacrine fluorescence spectra. (okstate.edu)
Cell Membrane1
- Glucose and KCl, which depolarize the cell membrane, as well as the Ca2+-mobilizing agonist, carbachol (CCh), cause substantial increases in [Ca2+]m which are associated with smaller rises in [Ca2+]c. (123dok.net)
MAChR1
- We tried to define simple paradigms to quantify routinely the efficacy of different mAChR agonists. (biomedcentral.com)
Glaucoma1
- Carbachol eyedrops are used to decrease the pressure in the eye for people with glaucoma. (wikipedia.org)
Bladder1
- Carbachol can also be used to stimulate bladder emptying to treat the condition of underactive bladder. (wikipedia.org)
Nicotine3
- Unlike acetylcholine and carbachol, nicotine uniquely induced drastic rearrangement of egg cortical microfilaments in a dose-dependent way. (mdpi.com)
- Relaxations of the isolated bovine retractor penis muscle elicited by nicotine and the three other nicotinic agonists acetylcholine, carbachol, and dimethylphenylpiperazinium were studied. (aspetjournals.org)
- Also carbachol and dimethylphenylpiperazinium induced relaxations qualitatively identical to those effected by the above-mentioned doses of nicotine. (aspetjournals.org)
Potency2
- These results demonstrate that the Ser388Tyr mutation is responsible for enhanced agonist potency and binding affinity, whereas the Thr389Pro mutation alters G protein interactions. (aspetjournals.org)
- Mutations of D105 in the orthosteric binding site and mutation of D99 located out of the orthosteric binding site decreased affinity of all tested agonists that was translated as a decrease in potency in accumulation of inositol phosphates and intracellular calcium mobilization. (cas.cz)
Inhibition3
- A direct correlation was observed between K p and the apparent inhibition constant (K i ) for agonists to displace AChR-bound quinacrine. (okstate.edu)
- By themselves, these results support the conjecture that agonist self-inhibition seems to be mediated by the quinacrine binding site via a membrane approach mechanism. (okstate.edu)
- however, we can not discard that the process of agonist self-inhibition can also be mediated by a steric blockage of the ion channel. (okstate.edu)
Asthma1
- Asthma: Choline esters (muscarinic agonists) can produce bronchoconstriction. (pharmacology2000.com)
Lipid1
- The calculated C M values indicated significant (between 7 and 54 mM) agonist accessibility to lipid membrane. (okstate.edu)
Currents2
- The metabolite quickly reversed short circuit currents (I sc ) stimulated by diverse agonists. (mcmaster.ca)
- We used undifferentiated PC-12 cells to study the effect of epinephrine and carbachol on transmembranous currents. (mdc-berlin.de)
Accumulation1
- The agonist-induced accumulation of [ -3 H]-myo-inositol-1-phosphate was dependent on tissue, lithium, [ 3 H]-myo-inositol concentration, as well as incubation time. (elsevierpure.com)
Effects4
- Zhang W, Tan YF, Atwood HL , Martin Wojtowicz J. Biphasic effects of the cholinergic agonist carbachol on long-term potentiation in the dentate gyrus of the mammalian hippocampus. (neurotree.org)
- Coronary vascular disease: Choline esters (muscarinic agonists), as a result of their hypotensive effects, can further compromise coronary blood flow. (pharmacology2000.com)
- The purpose of the present study was to determine whether carbacol, a cholinergic agonist, mimics the phase-shifting effects of light on the circadian rhythm of locomotor activity (CRLA) in the Djungarian hamster. (northwestern.edu)
- These results indicate that carbachol mimics some of the effects of light on the circadian system in the Djungarian hamster and support the hypothesis that cholinergic mechanisms may play a role in mediating some of the phase-shifting effects of light on the circadian clock of mammals. (northwestern.edu)
Significantly2
- In ligand binding experiments, mutation of Ser388Tyr resulted in significantly increased agonist binding affinity. (aspetjournals.org)
- This treatment did not significantly affect the response of the cells to carbachol. (edu.au)
Affinity1
- In contrast, mutation of Thr389Pro did not change agonist binding affinity but rendered multiple agonist binding sites, and the high-affinity binding was sensitive to GTP analogs. (aspetjournals.org)
Compound1
- Carbachol is a choline carbamate and a positively charged quaternary ammonium compound. (wikipedia.org)
Response3
- Because most tubulin is not membrane associated, this study investigates whether tubulin translocates to the membrane in response to an agonist so that it might regulate G-protein signaling. (jneurosci.org)
- The latter resulted in a marked amplification of the response to all agonists tested. (elsevierpure.com)
- No consistent phase shifts were observed in response to carbachol injections at other circadian times. (northwestern.edu)
Membranes1
- A specific and time-dependent association of tubulin with plasma membranes was observed when SK-N-SH cells were treated with carbachol. (jneurosci.org)
Drugs1
- Just like muscarinic agonists, anticholinergics act as examples for drugs bind to GPCR. (egpat.com)
Experiments1
- The agonist membrane partitioning experiments indicated relatively small (≤20) K p values relative to tetracaine. (okstate.edu)
Concentration1
Cells1
- In SK-N-SH cells, carbachol induced a rapid and transient translocation of tubulin to the plasma membrane, microtubule reorganization, and a change in cell shape as demonstrated by confocal immunofluorescence microscopy. (jneurosci.org)
Interact1
- The principal difference among the studied agonists is rather in the way they interact with D105 in the orthosteric binding site. (cas.cz)
Responses1
- In addition, the reconstructed tissues show contractile responses to potassium and carbachol. (basicmedicalkey.com)