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23062-91-1

23062-91-1 structure

23062-91-1 structure

Name: PD 102807
Chemical Name: pd 102807
CAS Number: 23062-91-1
Molecular Formula: C₂₃H₂₄N₂O₄
Molecular Weight: 392.45
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2016-06-11 12:11:23
Modify Date: 2026-07-09 19:47:08
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.

Name	pd 102807
Synonyms	Ethyl 9-methoxy-2-methyl-6a,11,12,14-tetrahydro-3H-indolo[4',5':5,6][1,3]oxazino[2,3-a]isoquinoline-1-cboxylate 3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1.2-b]pyrrolo[3.2-f]benzoxazine-1-cboxylicacidethyles] 3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-cboxylic acid ethyl ester 3,6A,11,14-TETRAHYDRO-9-METHOXY-2-METHYL-(12H)-ISOQUINO[1,2-B]PYRROLO[3,2-F][1,3]BENZOXAZINE-1-CBOXYLIC ACID, ETHYL ESTER hms3268m09 12H-Isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-cboxylic acid, 3,6a,11,14-tetrahydro-9-methoxy-2-methyl-, ethyl ester

Description	PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Neurological Disease
In Vitro	PD 102807 (example 1) shows selectivity for M4 muscarinic receptor with 72-fold (M1), 38-fold (M2), 10-fold (M3), and 82-fold (M5) more selective compared to the other receptors[1]. PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [35S]-GTPγS binding to membrane G proteins with a pKB of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pKB=5.60), M2 (pKB=5.88) and M3 (pKB=6.39) receptor subtypes, respectively[2]. PD-102807 is an M4 mAChR preferring antagonist, with 7-28 nM affinity for M4 mAChRs, a 14-36-fold selectivity for M4 over M3 mAChRs, and 76-2600-fold selectivity for M4 over M1, M2 and M5 mAChRs[3].
In Vivo	Striatal perfusion of PD-102807 (3 μM) alleviates levodopa-induced dyskinesia (LID) and inhibits nigral GABA and Glu along with striatal Glu release[3]. Animal Model: Male Sprague-Dawley rats[3] Dosage: 3 μM Administration: Administration:Perfusion started 40 min prior to L-DOPA (6 mg/Kg plus 12 mg/Kg benserazide, s.c.) administration and continued until the end of experiment. Result: Basal dialysate levels in PD-102807 experiment were 19.19±2.62 nM and 47.77±3.42 nM for GABA and Glu in SNr, respectively, and 41.38±4.25 nM for Glu in striatum. Reduced global Axial Limb Orolingual (ALO) Abnormal Involuntary Movements (AIM) expression from 70.75±5.64 to 25.38±6.64, significantly attenuating limb, axial and orolingual AIMs at 3 μM. Inhibited the L-DOPA-induced rise of substantia nigra pars reticulata (SNr) GABA, SNr Glu, and striatal Glu at 3 μM.
References	[1]. C E Augelli-Szafran, et al. Identification and characterization of m4 selective muscarinic antagonists. Bioorg Med Chem Lett. 1998 Aug 4;8(15):1991-6. [2]. M C Olianas, et al. 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. [3]. Alberto Brugnoli, et al. 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.

Density	1.34g/cm3
Boiling Point	586ºC at 760 mmHg
Molecular Formula	C₂₃H₂₄N₂O₄
Molecular Weight	392.45
Flash Point	308.2ºC
Exact Mass	392.17400
PSA	63.79000
LogP	4.04880
Vapour Pressure	1.02E-13mmHg at 25°C
Index of Refraction	1.673

110339-54-3 structure

110339-54-3

~%

23062-91-1 structure

23062-91-1

Literature: Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996

2039-67-0 structure

2039-67-0

~%

23062-91-1 structure

23062-91-1

Literature: Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996

7598-91-6 structure

7598-91-6

~%

23062-91-1 structure

23062-91-1

Literature: Augelli-Szafran, Corinne E.; Jaen, Juan C.; Moreland, David W.; Nelson, Carrie B.; Penvose-Yi, Jan R.; Schwarz, Roy D. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1991 - 1996

Precursor 3
110339-54-3 2039-67-0 7598-91-6
DownStream 0

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