Synonym
PD102807; PD 102807; PD-102807;
IUPAC/Chemical Name
Ethyl (S)-9-methoxy-2-propyl-3,6a,11,14-tetrahydro-12H-indolo[4',5':5,6][1,3]oxazino[2,3-a]isoquinoline-1-carboxylate
InChi Key
JCJXWNVOVZEIHE-DEOSSOPVSA-N
InChi Code
InChI=1S/C25H28N2O4/c1-4-6-19-23(25(28)30-5-2)22-18-14-27-12-11-15-13-16(29-3)7-8-17(15)24(27)31-21(18)10-9-20(22)26-19/h7-10,13,24,26H,4-6,11-12,14H2,1-3H3/t24-/m0/s1
SMILES Code
O=C(C1=C(CCC)NC2=C1C(C3)=C(C=C2)O[C@]4([H])N3CCC5=C4C=CC(OC)=C5)OCC
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
420.51
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Olianas MC, Onali P. PD 102807, a novel muscarinic M4 receptor antagonist, discriminates between striatal and cortical muscarinic receptors coupled to cyclic AMP. Life Sci. 1999;65(21):2233-40. doi: 10.1016/s0024-3205(99)00488-9. PMID: 10576595.
2: Brugnoli A, Pisanò CA, Morari M. Striatal and nigral muscarinic type 1 and type 4 receptors modulate levodopa-induced dyskinesia and striato-nigral pathway activation in 6-hydroxydopamine hemilesioned rats. Neurobiol Dis. 2020 Oct;144:105044. doi: 10.1016/j.nbd.2020.105044. Epub 2020 Aug 13. PMID: 32798726.
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5: Pujol Lereis VA, Hita FJ, Gobbi MD, Verdi MG, Rodriguez MC, Rothlin RP. Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein. Br J Pharmacol. 2006 Mar;147(5):516-23. doi: 10.1038/sj.bjp.0706654. PMID: 16444291; PMCID: PMC1616972.
6: Choppin A, Eglen RM. Pharmacological characterization of muscarinic receptors in dog isolated ciliary and urinary bladder smooth muscle. Br J Pharmacol. 2001 Feb;132(4):835-42. doi: 10.1038/sj.bjp.0703901. PMID: 11181424; PMCID: PMC1572633.
7: Lau BK, Vaughan CW. Muscarinic modulation of synaptic transmission via endocannabinoid signalling in the rat midbrain periaqueductal gray. Mol Pharmacol. 2008 Nov;74(5):1392-8. doi: 10.1124/mol.108.045872. Epub 2008 Aug 4. PMID: 18678620.
8: Böhme TM, Augelli-Szafran CE, Hallak H, Pugsley T, Serpa K, Schwarz RD. Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors. J Med Chem. 2002 Jul 4;45(14):3094-102. doi: 10.1021/jm011116o. Erratum in: J Med Chem 2002 Oct 10;45(21):4800. PMID: 12086495.
9: Myslivecek J, Klein M, Novakova M, Ricny J. The detection of the non-M2 muscarinic receptor subtype in the rat heart atria and ventricles. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):103-16. doi: 10.1007/s00210-008-0285-8. Epub 2008 Apr 29. PMID: 18443764.
10: Hogan K, Markos F. Muscarinic type 1 receptors mediate part of nitric oxide's vagal facilitatory effect in the isolated innervated rat right atrium. Nitric Oxide. 2007 Feb;16(1):110-7. doi: 10.1016/j.niox.2006.05.005. Epub 2006 Jun 7. PMID: 16843016.
