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Tests related to pathologies



Select the pathology Select the target Select the Pharma Ref.
Tests for

Addiction

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

mGluR2 receptors

DCG-IV

Pre-synaptic mGluR2 receptors

- Smialowska M, Wieronska JM, Domin H, Zieba B (2007). Neuropsychopharmacology 32:1242-1250.
- Swanson CJ, Bures M, Johnson MP, Linden AM, Monn JA, Schoepp DD (2005). Nat Rev Drug Discov 4:131-144.
- Zhao Y, Dayas CV, Aujla H, Baptista MA, Martin-Fardon R, Weiss F (2006). J Neurosci 26:9967-9974.

P-014

mGluR2-mediated depression of synaptic transmission at MPP synapses

Tests for

Alzheimer's Disease

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Acetylcholinesterase

Physostigmine (Eserine)

cholinergic modulation of glutamate neurotransmission

- Wilkinson, DG (1999), Expert Opin. Pharmacother., 1, 121-135.
- Colgin et al. (2003), J. Neurophysiol., 90, 2358-2366.
- Lleo, A et al. (2005), Annu. Rev. Med., 57, 513-533.
- Coulthard, E et al. (2006), Curr. Opin. Neurol., 19, 613-618.

P-010

Cholinergic transmission - Alzheimer's disease

NMDA & Nicotinic receptors

Memantine

Long-Term Potentiation / Memory

- Parsons, CG et al. (1993), Neuropharmacology, 32, 1337-1350.
- Parson, CG et al. (1996), Eur. J. Neurosci., 8, 446-454.
- Buisson & Bertrand (1998), Mol. Pharmacol., 53, 555-563.
- Lipton, SA (2004), NeuroRx, 1, 101-110.
- Ringman, JM & Cummings, JL (2006), Behav. Neurol., 17, 5-16.

P-011

NMDA & Nicotinic receptors / Alzheimer's & Parkinson's diseases

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

NMDA receptors

D-AP5

Pure NMDA-mediated EPSP

- M. R. Foy et al. (1999), J Neurophysiol 81:925-929.
- Duncan, GE et al. (1999) Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-020

NMDA receptor modulators

M1 Muscarinic acetylcholine receptors

Carbachol & Pirenzepine

CA1 pyramidal neurons spontaneous activity

Langmead CJ, Watson J, Reavill C (2008). Pharmacol Ther.
Feb;117(2):232-43. Review. - Caccamo A, Oddo S, Billings LM, Green KN, Martinez-Coria H, Fisher A, LaFerla FM (2006). Neuron Mar 2;49(5):671-82.
- Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D, Felder CC (2011). J Pharmacol Exp Ther, Aug;338(2):622-32.

P-023

Cholinergic receptors-mediated increase of CA1 pyramidal neurons firing

Tests for

Amyotrophic Lateral Sclerosis

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

AMPA/Kainate receptors

NBQX

Glutamatergic synaptic transmission

- Catarzi, D et al. (2006), Med. Res. Rev. 27, 239-278.
- Namba, T et al. (1994), Brain Res., 638, 36-44.
- Sheardown, MJ (1993), Stroke, 24, 146-147.

P-002

AMPA- mediated synaptic transmission

Tests for

Anxiety

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

GABA-A receptors

Bicuculline

Epileptiform activity

- Olsen RW, Ban M, Miller T (1976), Brain Res 102:283-299.
- Treiman DM (2001), Epilepsia, 42 Suppl 3, 8-12.

P-004

GABA-A receptors - Network Excitability

GABA-A receptors

Ganaxolone

Allosteric modulation of GABA-A

- Belelli & Lambert (2005), Nature Neurosci., 6, 565-575.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Stell, BM et al. (2003), Proc. Natl. Acad. Sci. (USA), 100, 14439-14444

P-005

Neurosteroids / GABA-A receptors

Phasic GABA-A receptors

Gabazin (SR-95531)

GABA-A receptor-mediated fast synaptic transmission

- Bai, D et al. (2001), Mol. Pharmacol., 59, 814-824.
- Stell, BM & Mody, I (2002), J. Neurosci., 22, RC223.
- Yeung, JF et al. (2003), Mol. Pharmacol., 63, 2-8.
- Semyanov et al. (2004), Trends Neurosci., 27, 262-269.
- Cossart, R. et al. (2005), Trends Neurosci., 28, 108-115.
- Farrant, M & Nusser, Z. (2005), Nat. Rev. Neuroci., 6, 215-229.

P-006

Inhibition of phasic GABA-A receptors

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

H1 and H2 Histamine receptors

Histamine

CA1 pyramidal neurons spontaneous activity

- Brown RE, Fedorov NB, Haas HL, Reymann KG (1995).
Neuropharmacology 34:181-190. - Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Haas HL, Greene RW (1986) Exp Brain Res 62:123-130.
- Selbach O, Brown RE, Haas HL (1997). Neuropharmacology 36:1539-1548.

P-013

Histamine receptors mediated increase of CA1 pyramidal neurons firing

mGluR2 receptors

DCG-IV

Pre-synaptic mGluR2 receptors

- Smialowska M, Wieronska JM, Domin H, Zieba B (2007). Neuropsychopharmacology 32:1242-1250.
- Swanson CJ, Bures M, Johnson MP, Linden AM, Monn JA, Schoepp DD (2005). Nat Rev Drug Discov 4:131-144.
- Zhao Y, Dayas CV, Aujla H, Baptista MA, Martin-Fardon R, Weiss F (2006). J Neurosci 26:9967-9974.

P-014

mGluR2-mediated depression of synaptic transmission at MPP synapses

GABA-A receptors

Diazepam

Paired-pulse inhibition

- Mühler H (2006), Cell Tissue Res., 326(2):505-16.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Wease KN, Davies SN (2005), BMC Neurosci., Nov 23;6:66.

P-021

GABAergic-mediated inhibition of synaptic transmission

Tests for

Cognitive Disorders

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

AMPA/Kainate receptors

Kainate

Excitotoxicity

- Dingledine, R et al. (1999), Pharm. Rev., 51, 7-61.
- Lynch, G (2004), Cur. Op. Pharmaco., 4, 4-11.
- Weiser, T (2005), Curr. Drug Targets CNS Neurol. Disord., 4, 153-159.
- Lerma, J (2006), Cur. Op. Pharmaco. 6, 89-97.
- Pinheiro, P & Mulle, C (2006), Cell Tissue Res., 326, 547-482.

P-008

AMPA/Kainate receptors-mediated excitotoxicity

L-type VDCC

Nifedipine

Modulation of synaptic transmission by VDCC

- O'Regan, MH et al. (1991), Exp. Brain Res., 84, 224-228.
- Disterhoft, JF et al. (1993), Clin. Neuropharmacol., 16 suppl.1, S12-S24.
- Catterall, WA (2000), Annu. Rev. Cell. Dev. Biol.,16, 521-555.
- Godukhin, O et al. (2002), Neuropharmacology, 42, 459-466.
- Bourinet, E & Zamponi, GW (2005), Curr. Top. Med. Chem., 5, 539-546.
- Striessnig, J et al. (2006), Biochem. Soc. Trans., 34, 903-909.

P-009

L-type calcium channels / Synaptic Transmission

Acetylcholinesterase

Physostigmine (Eserine)

cholinergic modulation of glutamate neurotransmission

- Wilkinson, DG (1999), Expert Opin. Pharmacother., 1, 121-135.
- Colgin et al. (2003), J. Neurophysiol., 90, 2358-2366.
- Lleo, A et al. (2005), Annu. Rev. Med., 57, 513-533.
- Coulthard, E et al. (2006), Curr. Opin. Neurol., 19, 613-618.

P-010

Cholinergic transmission - Alzheimer's disease

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

H1 and H2 Histamine receptors

Histamine

CA1 pyramidal neurons spontaneous activity

- Brown RE, Fedorov NB, Haas HL, Reymann KG (1995).
Neuropharmacology 34:181-190. - Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Haas HL, Greene RW (1986) Exp Brain Res 62:123-130.
- Selbach O, Brown RE, Haas HL (1997). Neuropharmacology 36:1539-1548.

P-013

Histamine receptors mediated increase of CA1 pyramidal neurons firing

D1/D5 Dopamine receptors

SCH23390

Dopaminergic modulation of synaptic transmission

- Frey U, Matthies H, Reymann KG, Matthies H (1991). Neurosci Lett 129:111-114.
- Huang YY, Kandel ER (1995). Proc Natl Acad Sci U S A 92:2446-2450.
- Lemon N, Manahan-Vaughan D (2006). J Neurosci 26:7723-7729.

P-015

Dopamine-induced increase of synaptic transmission and plasticity

Tests for

Dementia

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Acetylcholinesterase

Physostigmine (Eserine)

cholinergic modulation of glutamate neurotransmission

- Wilkinson, DG (1999), Expert Opin. Pharmacother., 1, 121-135.
- Colgin et al. (2003), J. Neurophysiol., 90, 2358-2366.
- Lleo, A et al. (2005), Annu. Rev. Med., 57, 513-533.
- Coulthard, E et al. (2006), Curr. Opin. Neurol., 19, 613-618.

P-010

Cholinergic transmission - Alzheimer's disease

NMDA & Nicotinic receptors

Memantine

Long-Term Potentiation / Memory

- Parsons, CG et al. (1993), Neuropharmacology, 32, 1337-1350.
- Parson, CG et al. (1996), Eur. J. Neurosci., 8, 446-454.
- Buisson & Bertrand (1998), Mol. Pharmacol., 53, 555-563.
- Lipton, SA (2004), NeuroRx, 1, 101-110.
- Ringman, JM & Cummings, JL (2006), Behav. Neurol., 17, 5-16.

P-011

NMDA & Nicotinic receptors / Alzheimer's & Parkinson's diseases

Tests for

Depression

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

L-type VDCC

Nifedipine

Modulation of synaptic transmission by VDCC

- O'Regan, MH et al. (1991), Exp. Brain Res., 84, 224-228.
- Disterhoft, JF et al. (1993), Clin. Neuropharmacol., 16 suppl.1, S12-S24.
- Catterall, WA (2000), Annu. Rev. Cell. Dev. Biol.,16, 521-555.
- Godukhin, O et al. (2002), Neuropharmacology, 42, 459-466.
- Bourinet, E & Zamponi, GW (2005), Curr. Top. Med. Chem., 5, 539-546.
- Striessnig, J et al. (2006), Biochem. Soc. Trans., 34, 903-909.

P-009

L-type calcium channels / Synaptic Transmission

Tests for

Epilepsy

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

AMPA/Kainate receptors

NBQX

Glutamatergic synaptic transmission

- Catarzi, D et al. (2006), Med. Res. Rev. 27, 239-278.
- Namba, T et al. (1994), Brain Res., 638, 36-44.
- Sheardown, MJ (1993), Stroke, 24, 146-147.

P-002

AMPA- mediated synaptic transmission

GABA-A receptors

Bicuculline

Epileptiform activity

- Olsen RW, Ban M, Miller T (1976), Brain Res 102:283-299.
- Treiman DM (2001), Epilepsia, 42 Suppl 3, 8-12.

P-004

GABA-A receptors - Network Excitability

GABA-A receptors

Ganaxolone

Allosteric modulation of GABA-A

- Belelli & Lambert (2005), Nature Neurosci., 6, 565-575.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Stell, BM et al. (2003), Proc. Natl. Acad. Sci. (USA), 100, 14439-14444

P-005

Neurosteroids / GABA-A receptors

Phasic GABA-A receptors

Gabazin (SR-95531)

GABA-A receptor-mediated fast synaptic transmission

- Bai, D et al. (2001), Mol. Pharmacol., 59, 814-824.
- Stell, BM & Mody, I (2002), J. Neurosci., 22, RC223.
- Yeung, JF et al. (2003), Mol. Pharmacol., 63, 2-8.
- Semyanov et al. (2004), Trends Neurosci., 27, 262-269.
- Cossart, R. et al. (2005), Trends Neurosci., 28, 108-115.
- Farrant, M & Nusser, Z. (2005), Nat. Rev. Neuroci., 6, 215-229.

P-006

Inhibition of phasic GABA-A receptors

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

AMPA/Kainate receptors

Kainate

Excitotoxicity

- Dingledine, R et al. (1999), Pharm. Rev., 51, 7-61.
- Lynch, G (2004), Cur. Op. Pharmaco., 4, 4-11.
- Weiser, T (2005), Curr. Drug Targets CNS Neurol. Disord., 4, 153-159.
- Lerma, J (2006), Cur. Op. Pharmaco. 6, 89-97.
- Pinheiro, P & Mulle, C (2006), Cell Tissue Res., 326, 547-482.

P-008

AMPA/Kainate receptors-mediated excitotoxicity

L-type VDCC

Nifedipine

Modulation of synaptic transmission by VDCC

- O'Regan, MH et al. (1991), Exp. Brain Res., 84, 224-228.
- Disterhoft, JF et al. (1993), Clin. Neuropharmacol., 16 suppl.1, S12-S24.
- Catterall, WA (2000), Annu. Rev. Cell. Dev. Biol.,16, 521-555.
- Godukhin, O et al. (2002), Neuropharmacology, 42, 459-466.
- Bourinet, E & Zamponi, GW (2005), Curr. Top. Med. Chem., 5, 539-546.
- Striessnig, J et al. (2006), Biochem. Soc. Trans., 34, 903-909.

P-009

L-type calcium channels / Synaptic Transmission

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

K+ channel

Phenytoin / Carbamazepine

In vitro epilepsy model

- Perreault P, Avoli M (1991). J Neurophysiol 65:771-785. - Traub RD, Colling SB, Jefferys JG (1995). J Physiol 489 ( Pt 1):127-140. - Yonekawa WD, Kapetanovic IM, Kupferberg HJ (1995). Epilepsy Res 20:137-150.

P-016

Model of 4-AP-induced epilepsy

NMDA receptor

Phenytoin / Carbamazepine

In vitro epilepsy model

- Arias RL, Bowlby MR (2005). Brain Res 1047:233-244.
- Armand V, Rundfeldt C, Heinemann U (2000) . Epilepsia 41:28-33.
- Tancredi V, Hwa GG, Zona C, Brancati A, Avoli M (1990) . Brain Res 511:280-290.

P-017

Model of low-magnesium-induced epilepsy

GABA-A receptor

Somatostatin

In vitro epilepsy model

- Debanne D, Thompson SM, Gühwiler BH.(2006) Epilepsia Feb;47(2):247-56.
- Tallent MK, Siggins GR (2007), J.physiol Apr;81(4):1626-35.
- Treiman DM (2001), Epilepsia, 42 Suppl 3, 8-12.

P-018

Model of bicuculline-induced epilepsy

GABA-A / M1muscarinic receptors

Diazepam

In vitro epilepsy model

- Behrends JC, ten Bruggencate G (1993). J Neurophysiol 69:626-629.
- Cruickshank JW, Brudzynski SM, McLachlan RS (1994). Brain Res 643:125-129.
- Harrison PK, Sheridan RD, Green AC, Scott IR, Tattersall JE (2004). J Pharmacol Exp Ther 310:678-686.
- McDonough JH, Jr., Zoeffel LD, McMonagle J, Copeland TL, Smith CD, Shih TM (2000). Epilepsy Res 38:1-14.

P-019

Model of cholinergic-induced epilepsy

GABA-A receptors

Diazepam

Paired-pulse inhibition

- Mühler H (2006), Cell Tissue Res., 326(2):505-16.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Wease KN, Davies SN (2005), BMC Neurosci., Nov 23;6:66.

P-021

GABAergic-mediated inhibition of synaptic transmission

NA

Kainate & Carbamazepine

CA1 pyramidal neurons spontaneous activity

- Day IP, Goudie J, Nishiki K, Williams PD (1995). Toxicol Lett. Apr;76(3):239-43.
- Easter A, Bell ME, Damewood JR Jr, Redfern WS, Valentin JP, Winter MJ, Fonck C, Bialecki RA.
(2009). Drug Discov Today.Sep;14(17-18):876-84. Jun 21. Review.
- Ketelaars SO, Gorter JA, van Vliet EA, Lopes da Silva FH, Wadman WJ. (2001). Neuroscience. 105(1):109-20.

P-022

Characterization of pro- or anti-convulsive properties

Tests for

Hungtington's Disease

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

NMDA receptors

D-AP5

Long-Term Potentiation

- Duncan, GE et al. (1999) Brain Res. Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-003

NMDA receptors competitive antagonist

Tests for

Hyperactivity and Attention Deficit Disorders

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

Acetylcholinesterase

Physostigmine (Eserine)

cholinergic modulation of glutamate neurotransmission

- Wilkinson, DG (1999), Expert Opin. Pharmacother., 1, 121-135.
- Colgin et al. (2003), J. Neurophysiol., 90, 2358-2366.
- Lleo, A et al. (2005), Annu. Rev. Med., 57, 513-533.
- Coulthard, E et al. (2006), Curr. Opin. Neurol., 19, 613-618.

P-010

Cholinergic transmission - Alzheimer's disease

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

Tests for

Ischemia

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

NMDA receptors

D-AP5

Pure NMDA-mediated EPSP

- M. R. Foy et al. (1999), J Neurophysiol 81:925-929.
- Duncan, GE et al. (1999) Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-020

NMDA receptor modulators

Tests for

Multiple Sclerosis

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

Tests for

Neurodegeneration

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

Tests for

Neuropathic Pain

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

Tests for

Obesity

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

Tests for

Obsessive-Compulsive Disorders

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

mGluR2 receptors

DCG-IV

Pre-synaptic mGluR2 receptors

- Smialowska M, Wieronska JM, Domin H, Zieba B (2007). Neuropsychopharmacology 32:1242-1250.
- Swanson CJ, Bures M, Johnson MP, Linden AM, Monn JA, Schoepp DD (2005). Nat Rev Drug Discov 4:131-144.
- Zhao Y, Dayas CV, Aujla H, Baptista MA, Martin-Fardon R, Weiss F (2006). J Neurosci 26:9967-9974.

P-014

mGluR2-mediated depression of synaptic transmission at MPP synapses

Tests for

Pain

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

Sodium channels

Tetrodotoxin

Action Potential genesis and propagation

- Meisler & Kearney (2005), J. Clin. Invest., 115, 2010-2017
- Jentsch, T. et al (2004), Nature Cell. Biol., 11, 1039-1047
- Devor, M. (2006), J. Pain, 7(1 Suppl 1), S31-S37

P-001

Fast sodium channel inhibition

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

AMPA/Kainate receptors

Kainate

Excitotoxicity

- Dingledine, R et al. (1999), Pharm. Rev., 51, 7-61.
- Lynch, G (2004), Cur. Op. Pharmaco., 4, 4-11.
- Weiser, T (2005), Curr. Drug Targets CNS Neurol. Disord., 4, 153-159.
- Lerma, J (2006), Cur. Op. Pharmaco. 6, 89-97.
- Pinheiro, P & Mulle, C (2006), Cell Tissue Res., 326, 547-482.

P-008

AMPA/Kainate receptors-mediated excitotoxicity

H1 and H2 Histamine receptors

Histamine

CA1 pyramidal neurons spontaneous activity

- Brown RE, Fedorov NB, Haas HL, Reymann KG (1995).
Neuropharmacology 34:181-190. - Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Haas HL, Greene RW (1986) Exp Brain Res 62:123-130.
- Selbach O, Brown RE, Haas HL (1997). Neuropharmacology 36:1539-1548.

P-013

Histamine receptors mediated increase of CA1 pyramidal neurons firing

Tests for

Parkinson's Disease

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

NMDA receptors

D-AP5

Long-Term Potentiation

- Duncan, GE et al. (1999) Brain Res. Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-003

NMDA receptors competitive antagonist

NMDA & Nicotinic receptors

Memantine

Long-Term Potentiation / Memory

- Parsons, CG et al. (1993), Neuropharmacology, 32, 1337-1350.
- Parson, CG et al. (1996), Eur. J. Neurosci., 8, 446-454.
- Buisson & Bertrand (1998), Mol. Pharmacol., 53, 555-563.
- Lipton, SA (2004), NeuroRx, 1, 101-110.
- Ringman, JM & Cummings, JL (2006), Behav. Neurol., 17, 5-16.

P-011

NMDA & Nicotinic receptors / Alzheimer's & Parkinson's diseases

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

D1/D5 Dopamine receptors

SCH23390

Dopaminergic modulation of synaptic transmission

- Frey U, Matthies H, Reymann KG, Matthies H (1991). Neurosci Lett 129:111-114.
- Huang YY, Kandel ER (1995). Proc Natl Acad Sci U S A 92:2446-2450.
- Lemon N, Manahan-Vaughan D (2006). J Neurosci 26:7723-7729.

P-015

Dopamine-induced increase of synaptic transmission and plasticity

NMDA receptors

D-AP5

Pure NMDA-mediated EPSP

- M. R. Foy et al. (1999), J Neurophysiol 81:925-929.
- Duncan, GE et al. (1999) Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-020

NMDA receptor modulators

Tests for

Schizophrenia

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

NMDA receptors

D-AP5

Long-Term Potentiation

- Duncan, GE et al. (1999) Brain Res. Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-003

NMDA receptors competitive antagonist

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

NMDA receptors

D-AP5

Pure NMDA-mediated EPSP

- M. R. Foy et al. (1999), J Neurophysiol 81:925-929.
- Duncan, GE et al. (1999) Brain Res. Rev., 29, 250-264.
- Malenka, RC & Nicoll, RA (1999), Science, 285, 1870-1874.
- Samanta, MK et al. (2006), Am. J. Ther., 13, 516-526.
- Bonuccelli, U & Del Dotto, P (2006), Neurology, 67(7 Suppl 2), S30-S38.

P-020

NMDA receptor modulators

GABA-A receptors

Diazepam

Paired-pulse inhibition

- Mühler H (2006), Cell Tissue Res., 326(2):505-16.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Wease KN, Davies SN (2005), BMC Neurosci., Nov 23;6:66.

P-021

GABAergic-mediated inhibition of synaptic transmission

M1 Muscarinic acetylcholine receptors

Carbachol & Pirenzepine

CA1 pyramidal neurons spontaneous activity

Langmead CJ, Watson J, Reavill C (2008). Pharmacol Ther.
Feb;117(2):232-43. Review. - Caccamo A, Oddo S, Billings LM, Green KN, Martinez-Coria H, Fisher A, LaFerla FM (2006). Neuron Mar 2;49(5):671-82.
- Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D, Felder CC (2011). J Pharmacol Exp Ther, Aug;338(2):622-32.

P-023

Cholinergic receptors-mediated increase of CA1 pyramidal neurons firing

Tests for

Sleep Disorders

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

GABA-A receptors

Bicuculline

Epileptiform activity

- Olsen RW, Ban M, Miller T (1976), Brain Res 102:283-299.
- Treiman DM (2001), Epilepsia, 42 Suppl 3, 8-12.

P-004

GABA-A receptors - Network Excitability

GABA-A receptors

Ganaxolone

Allosteric modulation of GABA-A

- Belelli & Lambert (2005), Nature Neurosci., 6, 565-575.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Stell, BM et al. (2003), Proc. Natl. Acad. Sci. (USA), 100, 14439-14444

P-005

Neurosteroids / GABA-A receptors

Phasic GABA-A receptors

Gabazin (SR-95531)

GABA-A receptor-mediated fast synaptic transmission

- Bai, D et al. (2001), Mol. Pharmacol., 59, 814-824.
- Stell, BM & Mody, I (2002), J. Neurosci., 22, RC223.
- Yeung, JF et al. (2003), Mol. Pharmacol., 63, 2-8.
- Semyanov et al. (2004), Trends Neurosci., 27, 262-269.
- Cossart, R. et al. (2005), Trends Neurosci., 28, 108-115.
- Farrant, M & Nusser, Z. (2005), Nat. Rev. Neuroci., 6, 215-229.

P-006

Inhibition of phasic GABA-A receptors

H3 Histamine receptor

R-alpha-methylhistamine

Pre-synaptic H3 receptor

- Brown RE, Reymann KG (1996). J Physiol 496 ( Pt 1):175-184.
- Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Esbenshade TA, Fox GB, Cowart MD (2006). Mol Interv 6:77-88, 59.
- Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). Trends Pharmacol Sci 25:618-625.
- Witkin JM, Nelson DL (2004). Pharmacol Ther 103:1-20.
- Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, Chen AS, Chen HY, Macneil DJ, Kanatani A, Tokita S (2006). Proc Natl Acad Sci U S A 103:13866-13871.

P-012

H3 Histamine receptor-dependent depression in Dentate Gyrus

H1 and H2 Histamine receptors

Histamine

CA1 pyramidal neurons spontaneous activity

- Brown RE, Fedorov NB, Haas HL, Reymann KG (1995).
Neuropharmacology 34:181-190. - Brown RE, Stevens DR, Haas HL (2001). Prog Neurobiol 63:637-672.
- Haas HL, Greene RW (1986) Exp Brain Res 62:123-130.
- Selbach O, Brown RE, Haas HL (1997). Neuropharmacology 36:1539-1548.

P-013

Histamine receptors mediated increase of CA1 pyramidal neurons firing

GABA-A receptors

Diazepam

Paired-pulse inhibition

- Mühler H (2006), Cell Tissue Res., 326(2):505-16.
- Rogawski, MA (2006), Epilepsy Res., 69, 273-294.
- Wease KN, Davies SN (2005), BMC Neurosci., Nov 23;6:66.

P-021

GABAergic-mediated inhibition of synaptic transmission

Tests for

Stroke

Target

Pharm.Ref

Biology

Bibliography

Code

Name

PDF

AMPA/Kainate receptors

NBQX

Glutamatergic synaptic transmission

- Catarzi, D et al. (2006), Med. Res. Rev. 27, 239-278.
- Namba, T et al. (1994), Brain Res., 638, 36-44.
- Sheardown, MJ (1993), Stroke, 24, 146-147.

P-002

AMPA- mediated synaptic transmission

mGluR1 & mGluR5 receptors

DHPG

LTD induced by mGluR1/mGluR5 activation

- Palmer, MJ et al. (1997), Neuropharmacology, 36, 1517-1532.
- Fitzjohn, SM et al. (2001), J. Physiol., 537, 421-430.
- Rammes, G et al. (2003), J. Physiol., 546 (Part 2), 455-460
- Gallagher, SM et al. (2004), J. Neurosci., 24, 4859-4864.
- Volk, LJ et al. (2006), J. Neurophysiol., 95, 2427-2438.
- Lea, PM & Faden, AI (2006), CNS Drug Rev., 12, 149-166.

P-007

DHPG - induced LTD

AMPA/Kainate receptors

Kainate

Excitotoxicity

- Dingledine, R et al. (1999), Pharm. Rev., 51, 7-61.
- Lynch, G (2004), Cur. Op. Pharmaco., 4, 4-11.
- Weiser, T (2005), Curr. Drug Targets CNS Neurol. Disord., 4, 153-159.
- Lerma, J (2006), Cur. Op. Pharmaco. 6, 89-97.
- Pinheiro, P & Mulle, C (2006), Cell Tissue Res., 326, 547-482.

P-008

AMPA/Kainate receptors-mediated excitotoxicity

L-type VDCC

Nifedipine

Modulation of synaptic transmission by VDCC

- O'Regan, MH et al. (1991), Exp. Brain Res., 84, 224-228.
- Disterhoft, JF et al. (1993), Clin. Neuropharmacol., 16 suppl.1, S12-S24.
- Catterall, WA (2000), Annu. Rev. Cell. Dev. Biol.,16, 521-555.
- Godukhin, O et al. (2002), Neuropharmacology, 42, 459-466.
- Bourinet, E & Zamponi, GW (2005), Curr. Top. Med. Chem., 5, 539-546.
- Striessnig, J et al. (2006), Biochem. Soc. Trans., 34, 903-909.

P-009

L-type calcium channels / Synaptic Transmission

 

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