PG-9 maleate

Presynaptic cholinergic modulator CAS# 155649-00-6

PG-9 maleate

Catalog No. BCC6779----Order now to get a substantial discount!

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Chemical structure

PG-9 maleate

3D structure

Chemical Properties of PG-9 maleate

Cas No. 155649-00-6 SDF Download SDF
PubChem ID 46905315 Appearance Powder
Formula C21H26BrNO6 M.Wt 468.34
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name (Z)-but-2-enedioic acid;(8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 2-(4-bromophenyl)propanoate
SMILES CC(C1=CC=C(C=C1)Br)C(=O)OC2CC3CCC(C2)N3C.C(=CC(=O)O)C(=O)O
Standard InChIKey VBUSCULTLLOSLM-BTJKTKAUSA-N
Standard InChI InChI=1S/C17H22BrNO2.C4H4O4/c1-11(12-3-5-13(18)6-4-12)17(20)21-16-9-14-7-8-15(10-16)19(14)2;5-3(6)1-2-4(7)8/h3-6,11,14-16H,7-10H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PG-9 maleate

DescriptionA potent analgesic and nootropic agent. Increases release of acetylcholine.

PG-9 maleate Dilution Calculator

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PG-9 maleate Molarity Calculator

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Preparing Stock Solutions of PG-9 maleate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1352 mL 10.676 mL 21.352 mL 42.704 mL 53.38 mL
5 mM 0.427 mL 2.1352 mL 4.2704 mL 8.5408 mL 10.676 mL
10 mM 0.2135 mL 1.0676 mL 2.1352 mL 4.2704 mL 5.338 mL
50 mM 0.0427 mL 0.2135 mL 0.427 mL 0.8541 mL 1.0676 mL
100 mM 0.0214 mL 0.1068 mL 0.2135 mL 0.427 mL 0.5338 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PG-9 maleate

Antinociceptive and antiamnesic properties of the presynaptic cholinergic amplifier PG-9.[Pubmed:9495837]

J Pharmacol Exp Ther. 1998 Mar;284(3):806-16.

The antinociceptive effect of 3 alpha-tropyl 2-(p-bromophenyl)propionate [(+/-)-PG-9] (10-40 mg kg-1 s.c.; 30-60 mg kg-1 p.o.; 10-30 mg kg-1 i.v.; 10-30 micrograms/mouse i.c.v.) was examined in mice, rats and guinea pigs by use of the hot-plate, abdominal-constriction, tail-flick and paw-pressure tests. (+/-)-PG-9 antinociception peaked 15 min after injection and then slowly diminished. The antinociception produced by (+/-)-PG-9 was prevented by the unselective muscarinic antagonist atropine, the M1-selective antagonists pirenzepine and dicyclomine and the acetylcholine depletor hemicholinium-3, but not by the opioid antagonist naloxone, the gamma-aminobutyric acidB antagonist 3-aminopropyl-diethoxy-methyl-phosphinic acid, the H3 agonist R-(alpha)-methylhistamine, the D2 antagonist quinpirole, the 5-hydroxytryptamine4 antagonist 2-methoxy-4-amino-5-chlorobenzoic acid 2-(diethylamino)ethyl ester hydrochloride, the 5-hydroxytryptamin1A antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine hydrobromide and the polyamines depletor reserpine. Based on these data, it can be postulated that (+/-)-PG-9 exerted an antinociceptive effect mediated by a central potentiation of cholinergic transmission. (+/-)-PG-9 (10-40 mg kg-1 i.p.) was able to prevent amnesia induced by scopolamine (1 mg kg-1 i.p.) and dicyclomine (2 mg kg-1 i.p.) in the mouse passive-avoidance test. Affinity profiles of (+/-)-PG-9 for muscarinic receptor subtypes, determined by functional studies (rabbit vas deferens for M1, guinea pig atrium for M2, guinea pig ileum for M3 and immature guinea pig uterus for putative M4), have shown an M4/M1 selectivity ratio of 10.2 that might be responsible for the antinociception and the anti-amnesic effect induced by (+/-)-PG-9 through an increase in acetylcholine extracellular levels. In the antinociceptive and antiamnesic dose range, (+/-)-PG-9 did not impair mouse performance evaluated by the rota-rod test and Animex apparatus.

Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters.[Pubmed:8201605]

J Med Chem. 1994 May 27;37(11):1704-11.

Previous studies have shown that (R)-(+)-hyoscyamine has analgesic activity as a consequence of increased ACh release following antagonism of central muscarinic autoreceptors. Since the enhancement of central cholinergic transmission could be beneficial for cognitive disorders, we manipulated (R)-(+)-hyoscyamine, synthesizing several derivatives of tropic and 2-phenylpropionic acids, with the aim of obtaining drugs which are able to increase ACh release and consequently to show analgesic and nootropic activities. The results showed that several new compounds are indeed potent analgesics (with an analgesic efficacy comparable to that of morphine) and that the most potent one ((+/-)-19, PG9) also has remarkable cognition-enhancing properties. Our study confirmed that the mechanism of action involves ACh release even if it is still unclear whether only muscarinic autoreceptors or, also, heteroreceptors are involved.

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