Protein Information

Name 5 HT2A
Synonyms 5 HT 2; 5 HT 2A; 5 HT2; 5 HT2A; 5 hydroxytryptamine (serotonin) receptor 2A; 5 hydroxytryptamine 2A receptor; 5 hydroxytryptamine receptor 2A; HTR 2…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
11868904 Kucukhuseyin C, Akbas N, Yillar DO: Effect of ondansetron on the contractile responses to positive inotropic agents in electrically driven left atria of rats. J Basic Clin Physiol Pharmacol. 2001;12(4):271-87.

We studied the interaction of ondansetron with positive inotropic agents, including serotonin (5-hydroxytryptophane, 5-HT), noradrenaline, 4-aminopyridine (4-AP), calcium chloride, or with reserpine in isolated electrically driven rat atria.
This result was considered as evidence for the participation of pre- and post-junctional 5-HT2A receptors and the involvement of the sympathetic nervous system in the positive inotropic action of 5-HT in rat atria.
3(0,0,0,3) Details
15602751 Wang SJ: Potential antidepressant LY 367265 presynaptically inhibits the release of glutamate in rat cerebral cortex. Synapse. 2005 Mar 1;55(3):156-63.

In this study, the effect of the potential antidepressant LY 367265, an inhibitor of the 5-hydroxytryptamine (5-HT) transporter and 5-HT2A receptor antagonist, on the release of endogenous glutamate was investigated in nerve terminals purified from rat cerebral cortex using an on-line enzyme-coupled fluorimetric assay.
LY 367265 inhibited the release of glutamate evoked by 4-aminopyridine (4AP) in a concentration-dependent manner; no effect was seen on KCl-evoked glutamate release.
2(0,0,0,2) Details
14976250 Bush E, Fielitz J, Melvin L, Martinez-Arnold M, McKinsey TA, Plichta R, Olson EN: A small molecular activator of cardiac hypertrophy uncovered in a chemical screen for modifiers of the calcineurin signaling pathway. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2870-5. Epub 2004 Feb 19.

In a high-throughput screen for small molecules capable of regulating MCIP1 expression in muscle cells, we identified a unique 4-aminopyridine derivative exhibiting an embedded partial structural motif of serotonin (5-hydroxytryptamine, 5-HT).
This molecule, referred to as pyridine activator of myocyte hypertrophy, acts as a selective agonist for 5-HT (2A/2B) receptors and induces hypertrophy of cardiac muscle cells through a signaling pathway involving calcineurin and a kinase-dependent mechanism that inactivates class II histone deacetylases, which act as repressors of cardiac growth.
2(0,0,0,2) Details
17016851 Wang SJ, Wang KY, Wang WC, Sihra TS: Unexpected inhibitory regulation of glutamate release from rat cerebrocortical nerve terminals by presynaptic 5-hydroxytryptamine-2A receptors. J Neurosci Res. 2006 Nov 15;84(7):1528-42.

DOI potently inhibited 4-aminopyridine (4AP)-evoked glutamate release.
4(0,0,0,4) Details
11739602 Lambe EK, Aghajanian GK: The role of Kv1.2-containing potassium channels in serotonin-induced glutamate release from thalamocortical terminals in rat frontal cortex. J Neurosci. 2001 Dec 15;21(24):9955-63.

Serotonin 5-HT (2A) receptors have been implicated in psychiatric illness and the psychotomimetic effects of hallucinogens.
Here, we investigate parallels in EPSCs induced by either serotonin or the potassium channel blockers 4-aminopyridine (4-AP) or alpha-dendrotoxin (DTX).
2(0,0,0,2) Details
11457791 Belohlavkova S, Simak J, Kokesova A, Hnilickova O, Hampl V: Fenfluramine-induced pulmonary vasoconstriction: role of serotonin receptors and potassium channels. J Appl Physiol. 2001 Aug;91(2):755-61.

A pharmacological blockade of K (V) channels by 4-aminopyridine (3 x 10 (-3) mol/l) markedly potentiated the pulmonary vasoconstrictor response to fenfluramine but was without effect on the reactivity to 5-HT.
Using isolated rat lungs perfused with Krebs-albumin solution, we compared the inhibitory effect of ritanserin, an antagonist of 5-HT (2) receptors, on fenfluramine- and 5-HT-induced vasoconstriction.
1(0,0,0,1) Details
18367171 Lee JJ, Hahm ET, Lee CH, Cho YW: 5-HT1A receptor-mediated activation of a G-protein-coupled inwardly rectifying K+ current in rat medial preoptic area neurons. Eur J Pharmacol. 2008 May 31;586(1-3):114-22. Epub 2008 Mar 4.


The 5-HT-activated K+ current was sensitively blocked by Ba2+, but not by 4-aminopyridine, and was completely suppressed by N-ethylmaleimide.
0(0,0,0,0) Details
11489454 Jeong HJ, Han SH, Min BI, Cho YW: 5-HT1A receptor-mediated activation of G-protein-gated inwardly rectifying K+ current in rat periaqueductal gray neurons. Neuropharmacology. 2001 Aug;41(2):175-85.


I5-HT was sensitive to K+ channel blockers such as quinine and Ba2+, but insensitive to 4-aminopyridine, Cs+ and tetraethylammonium.
0(0,0,0,0) Details