PTAC oxalate

Muscarinic receptor ligand; exhibits partial agonist and antagonist activity at different subtypes CAS# 201939-40-4

PTAC oxalate

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Chemical structure

PTAC oxalate

3D structure

Chemical Properties of PTAC oxalate

Cas No. 201939-40-4 SDF Download SDF
PubChem ID 90488949 Appearance Powder
Formula C14H21N3O4S2 M.Wt 359.46
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 3-[(5R,6R)-1-azabicyclo[3.2.1]octan-6-yl]-4-propylsulfanyl-1,2,5-thiadiazole;oxalic acid
SMILES CCCSC1=NSN=C1C2CN3CCCC2C3.C(=O)(C(=O)O)O
Standard InChIKey LXXQOVMTAFXOKQ-IYPAPVHQSA-N
Standard InChI InChI=1S/C12H19N3S2.C2H2O4/c1-2-6-16-12-11(13-17-14-12)10-8-15-5-3-4-9(10)7-15;3-1(4)2(5)6/h9-10H,2-8H2,1H3;(H,3,4)(H,5,6)/t9-,10-;/m0./s1
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 PTAC oxalate

DescriptionMuscarinic receptor ligand. Displays partial agonist activity at M2 and M4 receptors; exhibits antagonist effects at M1, M3 and M5 receptors (Ki values are 2.8, 0.2, 0.6, 0.2 and 0.8 nM respectively). Displays selectivity for muscarinic receptors over a range of neurotransmitter receptors and ion channels. Inhibits firing rate of dopaminergic cells in the limbic ventral tegmental area after acute administration, without binding to dopamine receptors.

PTAC oxalate Dilution Calculator

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PTAC oxalate Molarity Calculator

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Preparing Stock Solutions of PTAC oxalate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.782 mL 13.9098 mL 27.8195 mL 55.639 mL 69.5488 mL
5 mM 0.5564 mL 2.782 mL 5.5639 mL 11.1278 mL 13.9098 mL
10 mM 0.2782 mL 1.391 mL 2.782 mL 5.5639 mL 6.9549 mL
50 mM 0.0556 mL 0.2782 mL 0.5564 mL 1.1128 mL 1.391 mL
100 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.5564 mL 0.6955 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 PTAC oxalate

Towards a muscarinic hypothesis of schizophrenia.[Pubmed:17146471]

Mol Psychiatry. 2007 Mar;12(3):232-46.

Although the neurotransmitter dopamine plays a prominent role in the pathogenesis and treatment of schizophrenia, the dopamine hypothesis of schizophrenia fails to explain all aspects of this disorder. It is increasingly evident that the pathology of schizophrenia also involves other neurotransmitter systems. Data from many streams of research including pre-clinical and clinical pharmacology, treatment studies, post-mortem studies and neuroimaging suggest an important role for the muscarinic cholinergic system in the pathophysiology of schizophrenia. This review will focus on evidence that supports the hypothesis that the muscarinic system is involved in the pathogenesis of schizophrenia and that muscarinic receptors may represent promising novel targets for the treatment of this disorder.

Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats.[Pubmed:10411607]

J Pharmacol Exp Ther. 1999 Aug;290(2):901-7.

The purpose of our studies was to determine the effects of muscarinic receptor agonists on conditioned avoidance responding in the rat. Rats were trained to avoid or escape an electric shock delivered to the feet in a discrete trial procedure. The muscarinic receptor agonists pilocarpine and [2-ethyl-8-methyl-2,8-diazaspiro(4. 5)decane-1,3-dione] hydrochloride (RS86) and the cholinesterase inhibitor physostigmine all decreased the percentage of avoidance responses at doses that produced less than approximately 30% response failures. Similar results were obtained with the antipsychotic drugs haloperidol, trifluoperazine, chlorpromazine, and clozapine. However, the benzodiazepine anxiolytic diazepam did not decrease avoidance responding up to doses that produced ataxia. On the other hand, oxotremorine and arecoline decreased avoidance responding only by producing response failures, whereas aceclidine produced intermediate changes. The muscarinic receptor antagonists scopolamine, trihexyphenidyl, and benztropine were without effect when administered alone but antagonized the decreases in avoidance responding produced by pilocarpine and RS86. Scopolamine had little effect on the decreases in avoidance responding produced by haloperidol. The newer muscarinic receptor partial agonists or agonist/antagonists [R-(Z)-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2. 2]octane-3-acetonitrile] hydrochloride, talsaclidine, milameline, and xanomeline also produced dose-related decreases in avoidance responding. Our results demonstrate that muscarinic receptor agonists can decrease avoidance responding in a manner similar to dopamine-receptor antipsychotic drugs, suggesting that muscarinic receptor agonists may provide an alternative approach to the treatment of psychosis.

Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane .[Pubmed:9774240]

Eur J Pharmacol. 1998 Sep 4;356(2-3):109-19.

(5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3 .2.1]octane (PTAC) is a potent muscarinic receptor ligand with high affinity for central muscarinic receptors and no or substantially less affinity for a large number of other receptors or binding sites including dopamine receptors. The ligand exhibits partial agonist effects at muscarinic M2 and M4 receptors and antagonist effects at muscarinic M1, M3 and M5 receptors. PTAC inhibited conditioned avoidance responding, dopamine receptor agonist-induced behavior and D-amphetamine-induced FOS protein M5 expression in the nucleus accumbens without inducing catalepsy, tremor or salivation at pharmacologically relevant doses. The effect of PTAC on conditioned avoidance responding and dopamine receptor agonist-induced behavior was antagonized by the acetylcholine receptor antagonist scopolamine. The compound selectively inhibited dopamine cell firing (acute administration) as well as the number of spontaneously active dopamine cells (chronic administration) in the limbic ventral tegmental area (A10) relative to the non-limbic substantia nigra, pars compacta (A9). The results demonstrate that PTAC exhibits functional dopamine receptor antagonism despite its lack of affinity for the dopamine receptors and indicate that muscarinic receptor partial agonists may be an important new approach in the medical treatment of schizophrenia.

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