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MDL 72832 hydrochloride

ligand for 5-HT1A receptor, potent and selective CAS# 113777-40-5

MDL 72832 hydrochloride

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Chemical structure

MDL 72832 hydrochloride

3D structure

Chemical Properties of MDL 72832 hydrochloride

Cas No. 113777-40-5 SDF Download SDF
PubChem ID 45073438 Appearance Powder
Formula C22H31ClN2O4 M.Wt 422.95
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 5 mM in water
Chemical Name 8-[4-(2,3-dihydro-1,4-benzodioxin-3-ylmethylamino)butyl]-8-azaspiro[4.5]decane-7,9-dione;hydrochloride
SMILES C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCNCC3COC4=CC=CC=C4O3.Cl
Standard InChIKey GQGDGISNRPBRSG-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H30N2O4.ClH/c25-20-13-22(9-3-4-10-22)14-21(26)24(20)12-6-5-11-23-15-17-16-27-18-7-1-2-8-19(18)28-17;/h1-2,7-8,17,23H,3-6,9-16H2;1H
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 MDL 72832 hydrochloride

DescriptionA potent ligand at 5-HT1A receptors, with mixed agonist and antagonist properties. An agonist at post-synaptic 5-HT1A receptors.

MDL 72832 hydrochloride Dilution Calculator

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Preparing Stock Solutions of MDL 72832 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3643 mL 11.8217 mL 23.6435 mL 47.2869 mL 59.1086 mL
5 mM 0.4729 mL 2.3643 mL 4.7287 mL 9.4574 mL 11.8217 mL
10 mM 0.2364 mL 1.1822 mL 2.3643 mL 4.7287 mL 5.9109 mL
50 mM 0.0473 mL 0.2364 mL 0.4729 mL 0.9457 mL 1.1822 mL
100 mM 0.0236 mL 0.1182 mL 0.2364 mL 0.4729 mL 0.5911 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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Background on MDL 72832 hydrochloride

MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor with pIC50 value of 9.1 [1].

The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.

MDL 72832 hydrochloride is a potent and selective ligand for 5-HT1A receptor [1]. Also, MDL 72832 exhibited affinity with pKD values of 6.32 and 6.34 for 5-HT1C and 5-HT1D receptors, respectively [1].

In rats, MDL 72832 inhibited 8-OH-DPAT-induced cardiovascular effects. In guinea-pigs, 8-OH-DPAT inhibited the contraction of the field-stimulated guinea-pig ileum in a concentration-dependent way. While MDL 72832 inhibited 8-OH-DPAT-induced neuronal inhibition. MDL 72832 is a ligand for 5-HT1A receptor with mixed antagonist and agonist properties [1]. In pre-satiated rats, (+) -MDL 72832 (1.0 mg/kg) stimulated food intake and (-) -MDL 72832 (0.03 mg/kg) significantly increased food intake [2]. In rats, MDL 72832 increased postsynaptic 5-HT1A receptors mediating hypothermia and exhibited agonist property [3].

References:
[1].  Mir AK, Hibert M, Tricklebank MD, et al. MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors. Eur J Pharmacol, 1988, 149(1-2): 107-120.
[2].  Neill JC, Cooper SJ. MDL 72832, a selective 5-HT1A receptor ligand, stereospecifically increases food intake. Eur J Pharmacol, 1988, 151(2): 329-332.
[3].  Millan MJ, Rivet JM, Canton H, et al. Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. J Pharmacol Exp Ther, 1993, 264(3): 1364-1376.

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References on MDL 72832 hydrochloride

Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists.[Pubmed:8450471]

J Pharmacol Exp Ther. 1993 Mar;264(3):1364-76.

In this study, we examined the localization of the 5-hydroxytryptamine (5-HT)1A receptors mediating hypothermia in the rat, evaluated the pharmacological specificity of this response and examined the influence of a series of novel 5-HT1A receptor ligands upon core temperature. Administered s.c., 8-hydroxy-(2-di-n-propylamino)tetralin hydrobromide (8-OH-DPAT), an agonist at both pre- and postsynaptic 5-HT1A receptors, elicited pronounced hypothermia. In contrast, BMY 7378, which shows low efficacy at postsynaptic 5-HT1A receptors but high efficacy at presynaptic 5-HT1A receptors, elicited only mild hypothermia. Similarly, 8-OH-DPAT was more efficacious than BMY 7378 in eliciting corticosterone secretion, a response mediated by postsynaptic 5-HT1A receptors, whereas BMY 7378 was as efficacious as 8-OH-DPAT in inhibiting striatal accumulation of 5-hydroxytryptophan, a response mediated by presynaptic 5-HT1A receptors. These data suggest, by analogy, that postsynaptic 5-HT1A receptors mediate hypothermia, an interpretation supported by the observation that destruction of central 5-HT neurons with 5,7-dihydroxytryptamine failed to reduce 8-OH-DPAT-induced hypothermia (DIH). Agonists at 5-HT1B, 5-HT1C, 5-HT2 and/or 5-HT3 receptors did not elicit hypothermia, and drugs releasing 5-HT elicited hyperthermia. In contrast, DIH was fully mimicked by the novel 5-HT1A receptors agonists, eltoprazine, WY 48,723, MDL 72832, tandospirone, S 14671, S 14506 and WY 50,324, whereas the novel partial agonist, zalospirone, was less efficacious. DIH was blocked by (-)-alprenolol, (+/-)-pindolol and the novel beta-blocker, (-)-tertatolol, which also has high affinity for 5-HT1A receptors; in distinction, betaxolol and ICI 118,551, antagonists at beta-1 and beta-2 adrenoceptors, respectively, were inactive. Spiperone, NAN-190 and BMY 7378 also inhibited DIH whereas ritanserin, SCH 39166, raclopride and prazosin, antagonists at 5-HT2 receptors, D1 and D2 dopamine receptors and alpha-1 adrenoceptors, respectively, were inactive. The novel 5-HT1A antagonists, WAY 100,135, MDL 73005 EF and (very potently) SDZ 216-525 all blocked DIH. Potency for induction of hypothermia and inhibition of DIH correlated well with affinity for 5-HT1A binding sites. In conclusion, hypothermia is a highly specific and sensitive response to activation of postsynaptic 5-HT1A receptors. Furthermore, DIH is inhibited by their selective blockade. At postsynaptic 5-HT1A receptors mediating hypothermia, eltoprazine, WY 48,723, MDL 72832 and tandospirone are agonists, zalospirone is a partial agonist and (-)-tertatolol, WAY 100,135, MDL 73005 EF and SDZ 216-525 are antagonists.

MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors.[Pubmed:2840295]

Eur J Pharmacol. 1988 Apr 27;149(1-2):107-20.

In receptor binding assays (+/-)MDL 72832, 8-[4-(1,4-benzodioxan-2-ylmethylamino)butyl]-8-azaspiro++ +[4,5] decane-7,9-dione, was a potent (pIC50 9.1), selective and stereospecific ligand for central 5-HT1A recognition sites. In functional tests, (+/-)MDL 72832 and its S(-) and R(+) enantiomers blocked stereoselectively the 8-OH-DPAT-induced neuronal inhibition of the transmurally stimulated guinea-pig ileum and the cardiovascular effects of 8-OH-DPAT in anaesthetized rats. In contrast, (+/-)MDL 72832 and its enantiomers were exclusively '8-OH-DPAT-like' in their ability to fully and stereoselectively generalize to the 8-OH-DPAT discriminative stimulus and, in reserpinised rats, to induce forepaw treading and flat body posture. These results characterize (+/-)MDL 72832 as a potent, stereoselective ligand with mixed agonist and antagonist properties at central and peripheral 5-HT1A receptors. The similar stereoselective requirements for the recognition site and functional effects provides compelling evidence that the 5-HT1A recognition site is indeed a functional receptor.

Description

Potent 5-HT1A ligand

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