Protein Information

Name 5 HT3
Synonyms 5 HT 3; 5 hydroxytryptamine 3 receptor; serotonin receptor; HTR 3; HTR3; 5 HT3; 5 HT3A; 5 HT3R…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
12171579 Johnston GA: Medicinal chemistry and molecular pharmacology of GABA (C) receptors. . Curr Top Med Chem. 2002 Aug;2(8):903-13.

GABA (C) receptors belong to the nicotinicoid superfamily of ionotropic receptors that include nicotinic acetylcholine receptors, bicuculline-sensitive GABA (A) receptors, strychnine-sensitive glycine receptors and 5HT3 serotonin receptors.
31(0,1,1,1) Details
11380521 Patten D, Foxon GR, Martin KF, Halliwell RF: An electrophysiological study of the effects of propofol on native neuronal ligand-gated ion channels. Clin Exp Pharmacol Physiol. 2001 May-Jun;28(5-6):451-8.

To gain some insight into the effects of propofol at a range of native neuronal receptors, the present study has used an extracellular recording technique and determined its effects at GABA (A), 5-HT3, P2X and nicotinic acetylcholine (nACh) receptors of the rat isolated vagus nerve and the GABA (A) and strychnine-sensitive glycine receptor of the rat isolated optic nerve.
31(0,1,1,1) Details
15566307 Maksay G, Nemes P, Biro T: Synthesis of tropeines and allosteric modulation of ionotropic glycine receptors. J Physiol. 2002 Nov 1;544(Pt 3):727-39.

These (nor) tropeines inhibited [(3) H] strychnine binding to glycine receptors in synaptosomal membranes of rat spinal cord.
Displacing potencies were also measured for [(3) H] granisetron binding to 5-HT (3) type serotonin receptors of rat cerebral cortex.
2(0,0,0,2) Details
12204190 Jung ME, Lal H, Gatch MB: The discriminative stimulus effects of pentylenetetrazol as a model of anxiety: recent developments. table of contents.


Several classes of compounds can modulate the PTZ discriminative stimulus including 5-HT (1A), 5-HT (3), NMDA, glycine, and L-type calcium channel ligands.
1(0,0,0,1) Details
12404628 Breitinger HG, Becker CM: The inhibitory glycine receptor-simple views of a complicated channel. Chembiochem. 2002 Nov 4;3(11):1042-52.

The strychnine-sensitive glycine receptor is the principal mediator of fast inhibitory synaptic transmission in the mammalian spinal cord and brain stem.
As a member of the ligand-gated ion-channel family, it shares structural homology with the nicotinic acetylcholine, GABA (A/C) and serotonin 5-HT (3) receptors.
1(0,0,0,1) Details
14561923 Verbitsky M, Plazas PV, Elgoyhen AB: Functional expression and properties of a nicotinic alpha9/5-HT3A chimeric receptor. Neuroreport. 2003 Oct 27;14(15):1931-4.

It was blocked by methyllycaconitine, strychnine, atropine and nicotine, with the same rank order of potency as alpha9 receptors.
1(0,0,0,1) Details
19726200 Maksay G, Vincze Z, Nemes P: Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors. Bioorg Med Chem. 2009 Oct 1;17(19):6872-8. Epub 2009 Aug 20.

Tropine esters displaced [(3) H] strychnine binding to glycine receptors of rat spinal cord with low Hill slopes.
Affinities of three (nor) tropeines were different for glycine receptors but identical for 5-HT (3) receptors.
1(0,0,0,1) Details
9895039 Kostowski W, Bienkowski P: Discriminative stimulus effects of ethanol: neuropharmacological characterization. Neurosci Biobehav Rev. 2002 Jun;26(4):429-39.

The ethanol stimulus effect may be increased (i.e., stronger recognition) by N-cholinergic drugs (nicotine), dopaminergic drugs (apomorphine), and 5-HT3 receptor agonists (m-chlorophenylbiguanide).
Further, some antagonists of strychnine-insensitive glycine modulatory sites among the NMDA receptor complex (e.g., L-701,324) dose-dependently substitute for the ethanol discriminative stimulus.
1(0,0,0,1) Details
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. Alcohol. 1999 Jan;17(1):63-80.


The selective alpha7-containing nAChR (alpha7*nAChR) agonist choline (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.
0(0,0,0,0) Details
11691868 Neunlist M, Michel K, Reiche D, Dobreva G, Huber K, Schemann M: Glycine activates myenteric neurones in adult guinea-pigs. J Physiol. 2001 Nov 1;536(Pt 3):727-39.


Strychnine (300 nM) reversibly abolished the glycine-induced depolarisation and the Cl (-) channel blocker picrotoxin (100 microM) reduced the amplitude of the depolarisation by 55 +/- 5 %.
0(0,0,0,0) Details
9886686 Maksay G: Bidirectional allosteric modulation of strychnine-sensitive glycine receptors by tropeines and 5-HT3 serotonin receptor ligands. Neuropharmacology. 1998 Dec;37(12):1633-41.
162(2,2,2,2) Details
16687139 Jensen AA, Gharagozloo P, Birdsall NJ, Zlotos DP: Pharmacological characterisation of strychnine and brucine analogues at glycine and alpha7 nicotinic acetylcholine receptors. Eur J Pharmacol. 2006 Jun 6;539(1-2):27-33. Epub 2006 May 9.

Most strikingly, quaternization of strychnine and brucine with substituents possessing different steric and electronic properties completely eliminated the activity at the glycine receptors, whereas binding affinity to the alpha7/5-HT3 chimera was retained for the majority of the quaternary analogues.
113(1,2,2,3) Details
12651653 Koshizaki M, Kawamata M, Shimada SG, Saito Y, Collins JG: 5-HT3 receptors partially mediate halothane depression of spinal dorsal horn sensory neurons. Anesth Analg. 2003 Apr;96(4):1027-31

Serotonin subtype 3 (5-HT (3)) receptors belong to the same ligand-activated ion-channel family as gamma-aminobutyric acid type A- and strychnine-sensitive glycine receptors, so we examined the possible involvement of 5-HT receptor systems in halothane depression of spinal sensory neurons.
33(0,1,1,3) Details
9351519 Green MA, Halliwell RF: Selective antagonism of the GABA (A) receptor by ciprofloxacin and biphenylacetic acid. Br J Pharmacol. 1997 Oct;122(3):584-90.

Responses mediated by 5-HT3, nicotinic ACh and P2X receptors in the vagus nerve and strychnine-sensitive glycine receptors in the optic nerve were little or unaffected by ciprofloxacin (100 microM), BPAA (100 microM) or the combination of these drugs (both at 100 microM). 6.
32(0,1,1,2) Details
8894185 Green KA, Lambert JJ, Cottrell GA: Ligand-gated ion channels opened by 5-HT in molluscan neurones. Br J Pharmacol. 1996 Oct;119(3):602-8.

1. 5-Hydroxytryptamine (5-HT) activated a fast (70 ms to half maximum) and desensitizing inward current through non-selective channels conducting predominantly monovalent cations in neurons of Helix aspersa. 2. alpha-Methyl-5-HT was equipotent with 5-HT in activating this current, but the known selective agonists at vertebrate 5-HT3 receptors, 2-methyl-5-HT and arylbiguanides were ineffective (< 100 microM). 5-Methoxytryptamine which is inactive on vertebrate 5-HT3 receptors was a very weak agonist. 3.
The responses were also antagonized by the non-specific antagonists (+)-tubocurarine and strychnine. 4.
3(0,0,0,3) Details