Protein Information

Name mu opioid receptors
Synonyms MOR 1; MOR1; Mu opiate receptor; Mu opioid receptor; Mu type opioid receptor; OPRM; OPRM 1; OPRM1…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
10790157 Endo K, Yawo H: mu-Opioid receptor inhibits N-type Ca2+ channels in the calyx presynaptic terminal of the embryonic chick ciliary ganglion. J Physiol. 2000 May 1;524 Pt 3:769-81.

L-ENK reduced Delta [Ca2+] t even in the presence of 4-aminopyridine (4-AP), which blocks the transient K+ conductance during the falling phase of the presynaptic action potential.
3(0,0,0,3) Details
15893634 Zhu W, Pan ZZ: Mu-opioid-mediated inhibition of glutamate synaptic transmission in rat central amygdala neurons. Neuroscience. 2005;133(1):97-103.

Furthermore, the mu-opioid inhibition of the EPSC was blocked by 4-aminopyridine (4AP; 100 microM), a voltage-dependent potassium channel blocker, and by phospholipase A (2) inhibitors AACOCF (3) (10 microM) and quinacrine (10 microM).
Opioid peptide methionine-enkephalin (ME; 10 microM) produced a significant inhibition (38%) in the amplitude of evoked EPSCs, an action mimicked by the mu-opioid receptor agonist [D-Ala (2),N-MePhe (4),Gly-ol (5)]-enkephalin (DAMGO; 1 microM, 44%).
3(0,0,0,3) Details
19178556 Panuccio G, Curia G, Colosimo A, Cruccu G, Avoli M: Epileptiform synchronization in the cingulate cortex. Epilepsia. 2009 Mar;50(3):521-36. Epub 2008 Oct 30.

RESULTS: Bath-application of the convulsant 4-aminopyridine (4AP, 50 microM) induced both brief and prolonged periods of epileptiform synchronization resembling interictal- and ictal-like discharges, respectively.
Mu-opioid receptor activation abolished 4AP-induced ictal events and markedly reduced the occurrence of the pharmacologically isolated GABAergic synchronous potentials.
2(0,0,0,2) Details
16806307 Schoffelmeer AN, Hogenboom F, Wardeh G, De Vries TJ: Interactions between CB1 cannabinoid and mu opioid receptors mediating inhibition of neurotransmitter release in rat nucleus accumbens core. Neuropharmacology. 2006 Sep;51(4):773-81. Epub 2006 Jun 30.

To that end, receptor-mediated inhibition of depolarization (4-aminopyridine)-induced [3H] glutamate release and glutamate (NMDA) receptor-stimulated [14C] acetylcholine (ACh) and [3H] GABA release was studied in superfused NAc core slices.
2(0,0,0,2) Details
15488297 Hahm ET, Lee JJ, Min BI, Cho YW: Opioid inhibition of GABAergic neurotransmission in mechanically isolated rat periaqueductal gray neurons. Neurosci Res. 2004 Nov;50(3):343-54.

In addition, K (+) channels blockers, Ba (2+) or 4-aminopyridine, did not affect the DAMGO effect.
The present study indicates that activation of presynaptic mu-opioid receptors coupled to G-proteins inhibits GABA release through unknown intracellular mechanisms downstream of Ca (2+) influx.
1(0,0,0,1) Details
17628526 Mert T, Gunes Y, Gunay I: Role of 4-aminopyridine-sensitive potassium channels in peripheral antinociception. Eur J Pharmacol. 2007 Oct 31;572(2-3):138-41. Epub 2007 Jun 29.

However, the possible participation of 4-aminopyridine-sensitive K+ channels to local antinociception induced by tramadol, a mu opioid receptor agonist, and lidocaine, a local anaesthetic, has been less studied.
31(0,1,1,1) Details
12128008 Bergevin A, Girardot D, Bourque MJ, Trudeau LE: Presynaptic mu-opioid receptors regulate a late step of the secretory process in rat ventral tegmental area GABAergic neurons. Neuropharmacology. 2002 Jun;42(8):1065-78.

The inhibition of action potential-evoked IPSCs and of spontaneous and ionomycin-evoked mIPSCs by DAMGO was prevented by the K (+) channel blocker, 4-aminopyridine (4-AP).
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17804632 Miura M, Saino-Saito S, Masuda M, Kobayashi K, Aosaki T: Compartment-specific modulation of GABAergic synaptic transmission by mu-opioid receptor in the mouse striatum with green fluorescent protein-expressing dopamine islands. J Neurosci. 2007 Sep 5;27(36):9721-8.

These effects of MOR were mediated principally by 4-aminopyridine-sensitive K+ conductance via a cAMP-dependent pathway, which was further augmented by previous blockade of the protein kinase C cascade.
2(0,0,0,2) Details
11530219 Louvel J, Papatheodoropoulos C, Siniscalchi A, Kurcewicz I, Pumain R, Devaux B, Turak B, Esposito V, Villemeure JG, Avoli M: GABA-mediated synchronization in the human neocortex: elevations in extracellular potassium and presynaptic mechanisms. Neuroscience. 2001;105(4):803-13.

Field potential and extracellular [K (+)] ([K (+)](o)) recordings were made in the human neocortex in an in vitro slice preparation to study the synchronous activity that occurs in the presence of 4-aminopyridine (50 microM) and ionotropic excitatory amino acid receptor antagonists.
Application of medium containing low [Ca (2+)]/high [Mg (2+)] (n=3 slices), antagonism of the GABA (A) receptor (n=7) or mu-opioid receptor activation (n=4) abolished these events.
1(0,0,0,1) Details
14618675 Yang TT, Hung CF, Lee YJ, Su MJ, Wang SJ: Morphine inhibits glutamate exocytosis from rat cerebral cortex nerve terminals (synaptosomes) by reducing Ca2+ influx. Synapse. 2004 Feb;51(2):83-90.

Morphine, a mu-opioid agonist, suppressed the Ca (2+)-dependent release of glutamate that was evoked by exposing cerebrocortical synaptosomes to the potassium channel blocker 4-aminopyridine.
This may therefore indicate that mu-opioid receptor agonists have neuroprotective properties, especially in the excessive glutamate release that occurs under certain pathological conditions.
1(0,0,0,1) Details
11011003 Wagner EJ, Reyes-Vazquez C, Ronnekleiv OK, Kelly MJ: The role of intrinsic and agonist-activated conductances in determining the firing patterns of preoptic area neurons in the guinea pig. Brain Res. 2000 Oct 6;879(1-2):29-41.

A smaller percentage of POA neurons (29%) expressed a transient outward, A-type K (+) current that was antagonized by a high concentration of 4-aminopyridine (3 mM).
Moreover, POA neurons responded to bath application of the mu-opioid receptor agonist DAMGO (93%) or the GABA (B) receptor agonist baclofen (83%) with a membrane hyperpolarization or an outward current.
1(0,0,0,1) Details
16515840 Fujita T, Kumamoto E: Inhibition by endomorphin-1 and endomorphin-2 of excitatory transmission in adult rat substantia gelatinosa neurons. Neuroscience. 2006;139(3):1095-105. Epub 2006 Mar 3.

The endomorphin-1 and endomorphin-2 currents were reduced in amplitude by K+-channel inhibitors, Ba2+ (100 microM) and 4-aminopyridine (1 mM), and also by mu-opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (1 microM) to a similar extent.
32(0,1,1,2) Details
12460247 Barbarosie M, Louvel J, D'Antuono M, Kurcewicz I, Avoli M: Masking synchronous GABA-mediated potentials controls limbic seizures. Epilepsia. 2002 Dec;43(12):1469-79.

PURPOSE: We determined how CA3-driven interictal discharges block ictal activity generated in the entorhinal cortex during bath application of 4-aminopyridine (4AP, 50 microM).
Accordingly, ictal discharges along with GABA-mediated interictal potentials disappeared during GABAA-receptor blockade (n = 7) or activation of mu-opioid receptors that inhibit GABA release (n = 4).
1(0,0,0,1) Details