Metabotropic : Agonists and Antagonists

Metabotropic receptors act through a second messenger to modulate the actions of excitatory and inhibitory . Most metabotropic neuroreceptors are -coupled and have a much longer-lasting effect than ionotropic receptors. Compounds that modulate these neuroreceptors are available from Cayman. Glutamate Receptors Item No. Product Name Summary A selective, positive allosteric modulator of mGluR2 (EC s = 33.2 and 96 nM in rat and human, 11986 Biphenylindanone A 50 respectively)

11988 Cinnabarinic Acid A partial receptor agonist of mGlu4, effective at 100 µM

16792 Kynurenic Acid​ Antagonizes subunit ζ-1 (Ki = 5.4 µM)

14693 LY341495 A selective mGluR2 and mGluR3 antagonist (IC50s = 21 and 14 nM, respectively)

14961 MTEP (hydrochloride) A negative allosteric modulator of the mGlu5a receptor subtype (Ki = 42 nM; IC50 = 110 nM)

14411 (S)-3,5-DHPG mGluR1a and mGluR5a agonist (Ki = 0.9 and 3.9 µM, respectively)

Dopamine Receptors Item No. Product Name Summary

14598 Bromocriptine (mesylate) D2 receptor agonist (Ki = 2.5 nM)

10488 Bupropion (hydrochloride) A Dopamine and norepinephrine reuptake inhibitor (IC50 = 6.5 and 3.4 μM, respectively)

15622 GBR 12909 (hydrochloride) A Dopamine uptake inhibitor (IC50 = 1-51 nM)

16149 L-DOPA methyl ester (hydrochloride) A metabolic precursor of dopamine that crosses the blood-brain barrier

15631 SCH 23390 (hydrochloride) A Dopamine D1-like receptor subtypes D1 and D5 antagonist (Kis = 0.2 and 0.3 nM, respectively)

15067 (±)-SKF 81297 (hydrobromide) A selective agonist of the dopamine D1-like receptor (Ki = 1.9 nM)

11984 Sumanirole Maleate Dopamine D2 receptor agonist (Ki = 9 nM)

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JAN2015 1180 EAST ELLSWORTH ROAD · ANN ARBOR, MI 48108 · USA · [800] 364-9897 WWW.CAYMANCHEM.COM Serotonin Receptors Item No. Product Name Summary

A 5-HT2 receptor agonist (IC s = 0.77 and 1.5 nM in human and rat cerebral cortex homogenates, 10011546 AL 34662 50 respectively-1.5 nM)

1A 12059 Clozapine A partial agonist at the 5-HT receptor (pKi = 7)

16752 Palonosetron (hydrochloride)​ Selective antagonist of 5-HT3 (pKi = 10.4 in rat cortex)

10096 SB 242084 (hydrochloride) A 5-HT2C receptor antagonist (pKi = 9.0)

A 5-HT agonist (K = 3.9-31 nM); also acts as an antagonist for the 5-HT , 5-HT , and 5-HT 14692 Tegaserod Maleate 4 i 2A 2B 2C receptors (Ki = 32, 3.9, and 100 nM, respectively)

15936 Volinanserin A selective 5-HT2A antagonist (Ki = 0.36-0.85 nM)

14599 WAY-100635 Maleate A potent, silent antagonist of serotonin 5-HT1A receptors (IC50 = 2.2 nM; Ki = 0.8 nM)

15871 Zolmitriptan A 5-HT1B and 5-HT1D agonist (Kis = 2.2 and 0.92 nM, respectively)

Muscarinic Acetylcholine Receptors Item No. Product Name Summary Non-selective, competitive antagonist of the mAChR types M , M , M , M , and M (pKBs range from 12008 Atropine 1 2 3 4 5 8.9-9.8)

16214 Benztropine (mesylate) A centrally acting M1 mAChR antagonist (Ki = 0.59 nM in rat) A positive allosteric modulator of the M mAChR that reduces the concentration of acetylcholine 15393 BQCA 1 required to activate M1 A potent antagonist of the M mAChR (pK = 9.3); also has a high affinity for the M receptor (pK = 14574 4-DAMP 3 i 5 i 8.9) A long-acting mAChR antagonist that binds equally to human muscarinic M , M , and M receptors 15773 Tiotropium (bromide) 1 2 3 (Kds = 0.04, 0.02, and 0.01 nM, respectively) A competitive antagonist of mAChRs (K = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M through M , 15027 Tolterodine (tartrate) i 1 5 respectively)

16606 Tropicamide​ An M4 mAChR antagonist (pKi = 7.2 in chicken heart) A potent agonist of mAChRs (EC values are 0.3, 92.5, 5, 52, and 42 nM for M , M , M , M , and M , 10790 Xanomeline oxalate 50 1 2 3 4 5 respectively)

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JAN2015 1180 EAST ELLSWORTH ROAD · ANN ARBOR, MI 48108 · USA · [800] 364-9897 WWW.CAYMANCHEM.COM