The class of transmembrane acetylcholine receptors can be divided into two main groups: the muscarinic (metabotropic) and the nicotinergic (ionotropic) receptors. This as a result of the specific binding affinities once determined of the two types of receptors for muscarine and nicotine respectively[1],[2].  The latter type is classified as a ligand gated ion channel, since activation of this receptor allows sodium ions to enter a cells interior and potassium and/or calcium ions to exit (section Ion channels (Ligand gated, Cys-loop, cationic)[3]. Unlike the nicotinergic acetylcholine receptor, the muscarinic type is part of the family of G-protein coupled receptors (GPCR-A18). In general, muscarinic acetylcholine receptors are known to play highly important and diverse roles in many basic physiological processes including gastrointestinal, cardiovascular, motor, attention, learning, memory, pain, sleep, and other functions[4]. Four subtypes have been identified, localized and characterized (M1-M4), whereas a fifth member has been cloned (M5), yet its function has not been revealed completely[5],[6]. In order to facilitate the study of this most recent addition to the family of mACh receptors, Axon Medchem offers VU 0238429 (Axon 1786) as a  high affinity drug (EC50 of approximately 1.16 µM at M5) with >30-fold selectivity versus M1 and M3, and no M2 or M4 potentiator activity.

[1] The pharmacology of flaxedil with observations on certain analogs. Riker WF, Wescoe WC. Ann NY Acad Sci 1951, 54, 373–394.
[2] The Chemical Transmission of Nerve Action. O. Loewi. Nobel Lecture,December 12, 1936.
[3] Purves, Dale, George J. Augustine, David Fitzpatrick, William C. Hall, Anthony-Samuel LaMantia, James O. McNamara, and Leonard E. White (2008). Neuroscience. 4th ed.. Sinauer Associates. pp. 122–6. ISBN 978-0-87893-697-7.
[4] Cloning and Expression of the Human and Rat m5 Muscarinic Acetylcholine Receptor Genes. Bonner, T. I.; Young, A. C.; Brann, M. R.; Buckley, N. J. Neuron 1988, 1, 403–410.
[5] Muscarinic acetylcholine receptor subtypes: localization and structure/function. Brann MR, Ellis J, Jørgensen H, Hill-Eubanks D, Jones SV. Prog Brain Res. 1993, 98, 121-7.
[6] Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. Bridges TM, Marlo JE, Niswender CM, et al. J. Med. Chem. 2009, 52, 3445–8.

24 Item(s)

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Axon ID Name Description From price
3513 Bethanechol chloride Muscarinic receptor (mAChR) agonist €50.00
1146 Clozapine Atypical antipsychotic €45.00
2796 Clozapine N-oxide Muscarinic DREADD agonist €85.00
1289 GMC 1-109 Clozapine analog devoid of DA, 5-HT2, H1 and α1 affinities, but with high M1 affinity €125.00
2851 GMC 1-161 Clozapine analog with 5-HT2A, M1 and D2 affinity, devoid of D1 affinities €135.00
1152 GMC 1-165 Clozapine analog with 5-HT2A and M1 affinity, devoid of D1/D2 affinities €135.00
3280 JHU37152 Potent and CNS-active DREADD agonist €90.00
3281 JHU37160 Potent and CNS-active DREADD agonist €90.00
1679 MDL 201012 Muscarinic M3 antagonist €110.00
1298 Olanzapine Atypical antipsychotic €75.00
3505 Oxybutynin hydrochloride Competitive M1/M2/M3 mAChR antagonist €50.00
3286 Penehyclidine hydrochloride Anticholinergic drug €130.00
2463 TBPB Allosteric activator of the M1 acetylcholine receptor devoid of M2-M5 activity. €105.00
2049 Tolterodine L-tartrate Muscarinic receptor (mAChR) antagonist €60.00
3648 Trospium chloride Specific, orally active and competitive muscarinic receptor (mAChR) antagonist  Recently added €60.00
1988 VU 0029767 PAM of mAChR M1 that potentiates the agonistic effect of Ach €110.00
1483 VU 0152100 PAM of M4 mAChR €85.00
1786 VU 0238429 Selective PAM of M5 mAChR (CHRM5) €105.00
1787 VU 0255035 Selective M1 mAChR Antagonist €120.00
1703 VU 0357017 hydrochloride PAM of M1 mAChR €115.00
1943 VU 0365114 Selective PAM of M5 mAChR (CHRM5) €115.00
2739 VU 6008667 Selective NAM of M5 mAChR (CHRM5) €105.00
3271 VU0486846 Potent and highly selective PAM of M1 mAChR €165.00
1273 Zamifenacin fumarate Muscarinic M3 antagonist €130.00

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