| Name | acetylcholine receptor (protein family or complex) |
|---|---|
| Synonyms | Acetylcholine receptor; Acetylcholine receptors |
| Name | strychnine |
|---|---|
| CAS | strychnidin-10-one |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 7478257 | Lawoko G, Jarlebark L, Heilbronn E: Ligand-binding properties of an unusual nicotinic acetylcholine receptor subtype on isolated outer hair cells from guinea pig cochlea. Neurosci Lett. 1995 Jul 28;195(1):64-8. L-[3H] bound reversibly (estimated KD approximately 230 nM and Bmax approximately 5 x 10 (7)) with kinetic rate constants of association kappa-1 = 6.2 +/- 0.06 x 10 (4) min-1 nM-1 and dissociation kappa-1 = 0.23 +/- 0.003 min-1. [3H] Strychnine bound to OHC with a KD of 35 +/- 6 nM and Bmax = 2.6 +/- 0.5 x 10 (7), and binding increased 3-4 fold after membrane depolarization with 56.2 mM [K+], suggesting additional binding sites. |
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| 12423674 | Bradaia A, Trouslard J: Nicotinic receptors regulate the release of onto lamina X neurones of the rat spinal cord. Neuropharmacology. 2002 Nov;43(6):1044-54. Whole-cell patch clamp recordings were performed on neurones in the lamina X of rat spinal cord slices in order to characterize glycinergic synaptic currents and their modulation by nicotinic acetylcholine receptors. These currents reversed near the ion equilibrium potential and were blocked by strychnine (1 microM). |
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| 16075378 | Daly JW: Nicotinic agonists, antagonists, and modulators from natural sources. Cell Mol Neurobiol. 2005 Jun;25(3-4):513-52. Acetylcholine receptors were initially defined as nicotinic or muscarinic, based on selective activation by two natural products, and muscarine. Noncompetitive antagonists, such as the histrionicotoxins, various izidines, decahydroquinolines, spiropyrrolizidine oximes, pseudophrynamines, ibogaine, strychnine, cocaine, and sparteine have come from natural sources. |
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| 17894865 | Takeda D, Nakatsuka T, Gu JG, Yoshida M: The activation of nicotinic acetylcholine receptors enhances the inhibitory synaptic transmission in the deep dorsal horn neurons of the adult rat spinal cord. Mol Pain. 2007 Sep 25;3:26. |
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| 9927615 | Rothlin CV, Katz E, Verbitsky M, Elgoyhen AB: The alpha9 nicotinic acetylcholine receptor shares pharmacological properties with type A and type 3 serotonin receptors. Mol Pharmacol. 1999 Feb;55(2):248-54. Thus, the type A gamma-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type 3 serotonin receptor antagonist ICS-205,930 block -evoked currents in alpha9-injected Xenopus laevis oocytes with the following rank order of potency: strychnine > ICS-205,930 > bicuculline. |
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| 8710935 | Jakubik J, Bacakova L, Lisa V, el-Fakahany EE, Tucek S: Activation of muscarinic acetylcholine receptors via their allosteric binding sites. Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8705-9. We have now found that the muscarinic receptor allosteric modulators alcuronium, gallamine, and strychnine (acting in the absence of an agonist) alter the synthesis of cAMP in Chinese hamster ovary (CHO) cells expressing the M2 or the M4 subtype of muscarinic receptors in the same direction as the agonist carbachol. |
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| 9224827 | Jakubik J, Bacakova L, El-Fakahany EE, Tucek S: Positive cooperativity of and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol. 1997 Jul;52(1):172-9. Vincamine, strychnine, and alcuronium displayed fewer positive allosteric interactions with the agonists, but each allosteric modulator displayed positive cooperativity with at least one agonist on at least one muscarinic receptor subtype. |
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| 7954834 | Elgoyhen AB, Johnson DS, Boulter J, Vetter DE, Heinemann S: Alpha 9: an acetylcholine receptor with novel pharmacological properties expressed in rat cochlear hair cells. Cell. 1994 Nov 18;79(4):705-15. |
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| 11223279 | Holt JC, Lioudyno M, Athas G, Garcia MM, Perin P, Guth PS: The effect of proteolytic enzymes on the alpha9-nicotinic receptor-mediated response in isolated frog vestibular hair cells. Hear Res. 2001 Feb;152(1-2):25-42. the predominant efferent transmitter, acting on acetylcholine receptors of these hair cells ultimately inhibits and/or facilitates vestibular afferent firing. In agreement with alpha9nAChR pharmacology obtained in other hair cells, the response in saccular hair cells was reversibly antagonized by strychnine, curare, tetraethylammonium, and apamin. |
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| 12213259 | Wong JY, Ross SA, McColl C, Massalas JS, Powney E, Finkelstein DI, Clark M, Horne MK, Berkovic SF, Drago J: Proconvulsant-induced seizures in alpha (4) nicotinic acetylcholine receptor subunit knockout mice. Neuropharmacology. 2002 Jul;43(1):55-64. We investigated the response of alpha (4) nAChR subunit knockout mice to the (GABA) receptor antagonists; pentylenetetrazole (PTZ) and bicuculline (BIC), the glutamate receptor agonist kainic acid (KA), the glycine receptor antagonist strychnine and the K (+) channel blocker 4-aminopyridine (4-AP). |
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| 17192652 | Jakubik J, Dolezal V: Determinants of positive cooperativity between strychnine-like allosteric modulators and N-methylscopolamine at muscarinic receptors. J Mol Neurosci. 2006;30(1-2):111-2. It has been shown previously that the third extracellular loop (o3) and its vicinity play a critical role in allosteric modulation at muscarinic acetylcholine receptors (mAChRs) (Ellis et al., 1993; Krejci and Tucek, 2001; Buller et al., 2002). |
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| 16950410 | Abdin MJ, Morioka N, Morita K, Kitayama T, Kitayama S, Nakashima T, Dohi T: Analgesic action of on tibial nerve transection (TNT)-induced mechanical allodynia through enhancement of the glycinergic inhibitory system in spinal cord. Life Sci. 2006 Dec 3;80(1):9-16. Epub 2006 Aug 17. For example, the stimulation of nicotinic acetylcholine receptors (nAChRs) leads to an antinociceptive effect. Furthermore, pretreatment with strychnine, a glycine receptor antagonist, blocked the antinociception induced by RJR-2403, and |
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| 17234181 | Mascia MP, Bachis E, Obili N, Maciocco E, Cocco GA, Sechi GP, Biggio G: Thiocolchicoside inhibits the activity of various subtypes of recombinant (A) receptors expressed in Xenopus laevis oocytes. Eur J Pharmacol. 2007 Mar 8;558(1-3):37-42. Epub 2006 Dec 12. Thiocolchicoside inhibited the function of recombinant human strychnine-sensitive glycine receptors composed of the alpha1 subunit with a potency (median inhibitory concentration of 47 microM) lower than that apparent with recombinant (A) receptors. It also inhibited the function of human nicotinic acetylcholine receptors composed of the alpha4 and beta2 subunits, but this effect was only partial and apparent at high concentrations. |
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| 9861707 | Zhao FY, Roberts A: Assessing the roles of glutamatergic and cholinergic synaptic drive in the control of fictive swimming frequency in young Xenopus tadpoles. J Comp Physiol A. 1998 Dec;183(6):753-8. The components of synaptic drive were revealed by the local microperfusion of strychnine together with different excitatory antagonists. After blocking the nicotinic acetylcholine receptor, the mainly glutamatergic excitatory synaptic drive still changed with frequency. |
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| 8890920 | Wang H, Cui WY, Liu CG: Regulatory effects of acutely repeated treatment towards central muscarinic receptors. Life Sci. 1996;59(17):1415-21. Sensitivity of brain muscarinic acetylcholine receptors to the agonists was examined in tolerant animals which were developed by acutely repeated injections of In conscious rats, the dose-response curves of muscarinic agonists arecoline and pilocarpine, cholinesterase inhibitors soman and physostigmine rather than GABA receptor antagonist pentylenetetrazol or glycine receptor antagonist strychnine for producing EEG seizures were shifted leftwards by acutely repeated injections of |
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| 7952289 | Bahring R, Standhardt H, Martelli EA, Grantyn R: -activated currents of postnatal mouse retinal ganglion cells are blocked by and how specific are ion channels in immature neurons?. Eur J Neurosci. 1994 Jul 1;6(7):1089-99. The block was voltage-independent and persisted during coapplication with the nicotinic and muscarinic acetylcholine receptor antagonists D-tubocurarine and atropine. -induced currents of retinal ganglion cells were blocked by bicuculline, picrotoxin and Zn2+, as well as strychnine, and increased by pentobarbital, clonazepam and 3 alpha--5 alpha-pregnan-20-one. |
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| 19860810 | Chau P, Stomberg R, Fagerberg A, Soderpalm B, Ericson M: Glycine receptors involved in acamprosate's modulation of accumbal levels: an in vivo microdialysis study. Alcohol Clin Exp Res. 2010 Jan;34(1):32-8. Epub 2009 Oct 23. BACKGROUND: Glycine receptors (GlyRs) in the nucleus accumbens (nAc) and nicotinic acetylcholine receptors (nAChRs) in the ventral tegmental area (VTA) have been suggested to be involved in the positive reinforcing and elevating effects of Pretreatment either with 10 microM strychnine in the nAc or 100 microM mecamylamine in the VTA, completely antagonized the acamprosate-induced elevation of accumbal levels. |
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| 17357155 | Speranskiy K, Cascio M, Kurnikova M: Homology modeling and molecular dynamics simulations of the glycine receptor ligand binding domain. Proteins. 2007 Jun 1;67(4):950-60. In addition, a complex structure with strychnine antagonist in the putative binding site is proposed based on docking simulation using Autodock program. Molecular dynamics (MD) simulations with simulated annealing protocol are reported on the proposed LBD of GlyR, which is stable in 5 ns simulation in water, as well as for a deformed LBD structure modeled on the corresponding domain determined in low-resolution cryomicroscopy structure of the alpha subunit of the full-length acetylcholine receptor (AChR). |
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| 17011596 | Zhao X, Marszalec W, Toth PT, Huang J, Yeh JZ, Narahashi T: In vitro galantamine-memantine co-application: mechanism of beneficial action. Neuropharmacology. 2006 Dec;51(7-8):1181-91. Epub 2006 Sep 29. Since Alzheimer's disease is known to be associated with down-regulation of the cholinergic and systems, most of these drugs inhibit acetylcholinesterase, potentiate the activity of nicotinic acetylcholine receptors (nAChRs), or modulate NMDA receptors. |
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| 12411519 | Bradaia A, Trouslard J: Fast synaptic transmission mediated by alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in lamina X neurones of neonatal rat spinal cord. J Physiol. 2002 Nov 1;544(Pt 3):727-39. The selective alpha7-containing nAChR (alpha7*nAChR) agonist (10 mM) induced a fast, rapidly desensitizing inward current, which was fully blocked by alpha-bungarotoxin (alpha-BgT; 50 nM) and strychnine (1 microM), two antagonists of alpha7*nAChRs. |
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| 8241451 | Bartolami S, Ripoll C, Eybalin M: Anticholinergic effects of strychnine in the cochlea do not involve muscarinic receptors. Neuroreport. 1993 Aug;4(8):1003-6. Central control of cochlear function is mediated by the cholinergic (medial) efferent system and both muscarinic and nicotinic acetylcholine receptors are thought to be present on outer hair cells. |
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| 19523966 | Mok MH, Fricker AC, Weil A, Kew JN: Electrophysiological characterisation of the actions of at ligand-gated ion channels. Neuropharmacology. 2009 Sep;57(3):242-9. Epub 2009 Jun 11. To better understand the effects of the metabolite (kynA) in the brain, we characterised its actions at five ligand-gated ion channels: AMPA, (A), and alpha7 nicotinic acetylcholine receptors. KynA inhibited AMPA-evoked currents to a similar degree in cultured hippocampal neurons and a human GluR2 (flip/unedited) cell line (IC (50): 433 and 596 muM, respectively) and at higher concentrations, kynA also inhibited the strychnine-sensitive glycine receptor ( approximately 35% inhibition by 3 mM kynA). |
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| 16678861 | Seddik R, Schlichter R, Trouslard J: Modulation of GABAergic synaptic transmission by terminal nicotinic acetylcholine receptors in the central autonomic nucleus of the neonatal rat spinal cord. Neuropharmacology. 2006 Jul;51(1):77-89. Epub 2006 May 5. The presynaptic effect of was blocked by 1microM of dihydro-beta-erythroidine (DHbetaE), an antagonist of non-alpha7 nAChRs but was insensitive to alpha7 nAChRs antagonists (strychnine, alpha-bungarotoxin and methyllycaconitine) or to the muscarinic receptor antagonist atropine (10microM). |
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| 11160606 | Ferreira M, Ebert SN, Perry DC, Yasuda RP, Baker CM, Davila-Garcia MI, Kellar KJ, Gillis RA: Evidence of a functional alpha7-neuronal nicotinic receptor subtype located on motoneurons of the dorsal motor nucleus of the vagus. J Pharmacol Exp Ther. 2001 Feb;296(2):260-9. In vitro autoradiography using 125I-alpha-bungarotoxin (alpha-BGTx) and anti-alpha7 immunohistochemistry were performed on the dorsal motor nucleus of the vagus (DMV) of sham and chronically vagotomized rats to determine whether the alpha7-nicotinic acetylcholine receptor (nAChR) is located postsynaptically on DMV neurons whose axons contribute to the vagus nerve. To test whether the alpha7-nAChR is similar to the alpha7-homomeric nAChR, experiments were performed in anesthetized rats, and compounds were microinjected into the DMV while monitoring intragastric pressure (IGP). alpha-BGTx and strychnine antagonized -induced increases in IGP; no antagonism was observed with methyllycaconitine, a compound known to block the homomeric alpha7-nAChR subtype. |
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| 8845730 | Heilbronn E, Jarlebark L, Lawoko G: Cholinergic and purinergic signalling in outer hair cells of mammalian cochlea. Neurochem Int. 1995 Oct-Nov;27(4-5):301-11. Strychnine, a glycine receptor blocker suggested to interfere with cholinergic sites of the efferent OHC synapse, was found to bind to OHC (cold strychnine for unspecific binding). In vivo and in vitro information is presented on structure, pharmacology, function and localization of the pre- and postsynaptic acetylcholine receptors (AChRs) at the efferent synapse. |
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| 8847100 | Hochstrate P, Schlue WR: Ca2+ influx into leech neuropile glial cells mediated by nicotinic acetylcholine receptors. Glia. 1995 Sep;15(1):43-53. In neuropile glial cells, cholinergic agonists induced a marked increase in [Ca2+] i that was inhibited by d-tubocurarine, alpha-bungarotoxin, strychnine, and atropine. |
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| 19087161 | Mochida H, Sato K, Momose-Sato Y: Switching of the transmitters that mediate hindbrain correlated activity in the chick embryo. Eur J Neurosci. 2009 Jan;29(1):14-30. Epub 2008 Dec 12. This finding sheds more light on the role of nicotinic acetylcholine receptors in the generation of correlated wave activity, which is considered to regulate the development of the nervous system. |
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| 9482782 | Guo JZ, Tredway TL, Chiappinelli VA: and release are enhanced by different subtypes of presynaptic nicotinic receptors in the lateral geniculate nucleus. J Neurosci. 1998 Mar 15;18(6):1963-9. The functional role of nicotinic acetylcholine receptors (nAChRs) in the ventral lateral geniculate nucleus (LGNv) was examined in chick brain slices. Methyllycaconitine and strychnine, other blockers of nAChRs containing the alpha7 subunit, failed to inhibit carbachol's increase of spontaneous glutamatergic and GABAergic PSCs. |
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| 9495848 | Matsubayashi H, Alkondon M, Pereira EF, Swanson KL, Albuquerque EX: Strychnine: a potent competitive antagonist of alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in rat hippocampal neurons. J Pharmacol Exp Ther. 1998 Mar;284(3):904-13. |
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| 7834198 | Kuijpers GA, Vergara LA, Calvo S, Yadid G: Inhibitory effect of strychnine on acetylcholine receptor activation in bovine medullary chromaffin cells. Br J Pharmacol. 1994 Oct;113(2):471-8. These results suggest that strychnine interacts with the agonist binding site of the nicotinic acetylcholine receptor in chromaffin cells, thus exerting a pharmacological effect independently of the glycine receptor. |
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| 8813554 | Proska J, Tucek S: Positive allosteric action of eburnamonine on cardiac muscarinic acetylcholine receptors. Eur J Pharmacol. 1996 Jun 3;305(1-3):201-5. It was discovered recently that alcuronium and strychnine (which is a precursor of alcuronium) allosterically increase the affinity of cardiac muscarinic receptors for the antagonist, N-methylscopolamine. |
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| 16421212 | Bray C, Son JH, Meizel S: causes an increase of intracellular in human sperm. . Mol Hum Reprod. 2005 Dec;11(12):881-9. Epub 2006 Jan 18. Sperm nicotinic acetylcholine receptors (nAChRs) can influence motility and the initiation of acrosome reaction (AR). Pre-incubation with 50 microM 3-quinuclidinyl benzilate (QNB) or 50 nM strychnine failed to inhibit the -initiated AR, demonstrating that muscarinic AChRs and nAChRs containing alpha9 subunits do not mediate this event. |
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| 15654288 | Molander A, Soderpalm B: Accumbal strychnine-sensitive glycine receptors: an access point for to the brain reward system. Alcohol Clin Exp Res. 2005 Jan;29(1):27-37. |
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| 10097172 | Garcia-Colunga J, Miledi R: Modulation of nicotinic acetylcholine receptors by strychnine. . Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):4113-8. |
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| 17900376 | Renna JM, Strang CE, Amthor FR, Keyser KT: Strychnine, but not PMBA, inhibits neuronal nicotinic acetylcholine receptors expressed by rabbit retinal ganglion cells. Vis Neurosci. 2007 Jul-Aug;24(4):503-11. However, other studies have shown that strychnine, in the concentrations commonly used, is also a potent competitive antagonist of alpha7 nicotinic acetylcholine receptors (nAChRs; Matsubayashi et al., 1998). |
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| 9986715 | Gharagozloo P, Lazareno S, Popham A, Birdsall NJ: Allosteric interactions of quaternary strychnine and brucine derivatives with muscarinic acetylcholine receptors. J Med Chem. 1999 Feb 11;42(3):438-45. |
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| 15878942 | Goutman JD, Fuchs PA, Glowatzki E: Facilitating efferent inhibition of inner hair cells in the cochlea of the neonatal rat. J Physiol. 2005 Jul 1;566(Pt 1):49-59. Epub 2005 May 5. Evoked IPSCs had biphasic waveforms at -60 mV, were blocked reversibly by alpha-bungarotoxin and strychnine and are most likely mediated by the alpha9/alpha10 acetylcholine receptor, with subsequent activation of -dependent (SK2) channels. |
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| 14742688 | Baker ER, Zwart R, Sher E, Millar NS: Pharmacological properties of alpha 9 alpha 10 nicotinic acetylcholine receptors revealed by heterologous expression of subunit chimeras. Mol Pharmacol. 2004 Feb;65(2):453-60. In agreement with evidence that alpha9alpha10 nAChRs exhibit an atypical pharmacological profile, we have identified specific high-affinity binding of several non-nicotinic ligands including strychnine (a glycine receptor antagonist), bicuculline (a GABAA receptor antagonist), and atropine (a muscarinic acetylcholine receptor antagonist). |
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| 16810300 | Kurzen H, Henrich C, Booken D, Poenitz N, Gratchev A, Klemke CD, Engstner M, Goerdt S, Maas-Szabowski N: Functional characterization of the epidermal cholinergic system in vitro. J Invest Dermatol. 2006 Nov;126(11):2458-72. Epub 2006 Jun 29. Blocking of all acetylcholine receptors (AChRs) by combined treatment with mecamylamine and atropine or treatment with strychnine (blocking alpha9nAChR) for 7-14 days resulted in a complete inhibition of epidermal differentiation and proliferation. |
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| 19861413 | Vogel N, Kluck CJ, Melzer N, Schwarzinger S, Breitinger U, Seeber S, Becker CM: Mapping of disulfide bonds within the amino-terminal extracellular domain of the inhibitory glycine receptor. J Biol Chem. 2009 Dec 25;284(52):36128-36. Epub 2009 Oct 27. The strychnine-sensitive glycine receptor (GlyR) is a ligand-gated chloride channel and a member of the superfamily of loop (Cys-loop) neurotransmitter receptors, which also comprises the nicotinic acetylcholine receptor (nAChR). |
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| 16687139 | Jensen AA, Gharagozloo P, Birdsall NJ, Zlotos DP: Pharmacological characterisation of strychnine and brucine analogues at and alpha7 nicotinic acetylcholine receptors. Eur J Pharmacol. 2006 Jun 6;539(1-2):27-33. Epub 2006 May 9. |
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| 19860809 | Chau P, Hoifodt-Lido H, Lof E, Soderpalm B, Ericson M: Glycine receptors in the nucleus accumbens involved in the intake-reducing effect of acamprosate. Alcohol Clin Exp Res. 2010 Jan;34(1):39-45. Epub 2009 Oct 23. BACKGROUND: We have previously demonstrated that strychnine-sensitive glycine receptors (GlyRs) in the nucleus accumbens (nAc) and nicotinic acetylcholine receptors (nAChRs) in the ventral tegmental area are involved in mediating (EtOH)-induced elevation of in the rat mesolimbic system. |
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| 15309481 | Wustenberg DG, Grunewald B: Pharmacology of the neuronal nicotinic acetylcholine receptor of cultured Kenyon cells of the honeybee, Apis mellifera. J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 2004 Oct;190(10):807-21. Epub 2004 Aug 11. The non-cholinergic drugs strychnine, bicuculline and picrotoxin partially and reversibly blocked the -induced currents. |
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