Effects of the alpha- and gamma-polymorphs of glycine on the behavior of catalepsy prone rats

Markel, A. L.; Achkasov, A. F.; Алехина, Т. А.; Prokudina, O. I.; Ryazanova, M. A.; Ukolova, T. N.; Ефимов, В. М.; Boldyreva, Elena V.; Болдырев, В. В.

doi:10.1016/j.pbb.2010.12.025

Cited by 24 publications

(19 citation statements)

References 37 publications

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“…It was reported that Nim was a substrate for cytochrome P450 (CYP) enzymes 24 , 25 . Moreover, as Markel et al 26 reported, γ -glycine had higher biological activity than α -glycine in ameliorating the behavioral disorders in the genetic catalepsy strain after oral administration of two glycine crystals. They concluded that this result may be related to differences in the supramolecular complexes formed during the interaction of the two polymorphs with biological liquids and the drug receptors.…”

Section: Discussionmentioning

confidence: 90%

Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration

Liu

Wang

Chen

et al. 2016

Acta Pharmaceutica Sinica B

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The previous investigation has proved that their existed pharmacokinetic difference between the different crystal forms of the polymorphic drugs after oral administration. However, no systemic investigations have been made on the change of this pharmacokinetic difference, resulted either from the physiological or from the pathological factors. In this paper, we used polymorphic nimodipine (Nim) as a model drug and investigated the effect of age difference (2- and 9-month old) on the pharmacokinetics after oral delivery in rats. As the results shown, for L-form of Nim (L-Nim), the AUC0–24 h in 2-month-old rats was 343.68±47.15 ng·h/mL, which is 23.36% higher than that in 9-month-old rats. For H-form of Nim (H-Nim), the AUC0–24 h in 2-month-old rats was 140.91±19.47 ng·h/mL, which is 54.64% higher than that in 9-month-old rats. The AUC0–24 h ratio between H-Nim and L-Nim was 2.44 in 2-month-old rats and 3.06 in 9-month-old rats. Since age difference could result in unparallelled change of the absorption and bioavailability of the polymorphic drugs, the results in this experiment are of value for further investigation of crystal form selection in clinical trials and rational clinical application of the polymorphic drugs.

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Section: Discussionmentioning

confidence: 90%

Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration

Liu

Wang

Chen

et al. 2016

Acta Pharmaceutica Sinica B

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“…It is being used by practical medical doctors as a neuroprotector in the acute period of ischemic stroke, [288][289][290] a protector in cisplatin nephrotoxicity, [293] a corrective medication against alcoholic intoxication, [294,295] and even to correct the functional states resulting from opium addiction. [296] Glycine can reduce the duration of cataleptic states, [297][298][299] enduring other negative symptoms of schizophrenia, [300][301][302][303][304] of bipolar disorders, [305] or different forms of dementia, including the Alzheimer's disease. [306] Its effect on the brain [307,308] is quite remarkable, considering that amino acids, including glycine, are abundant in the body as a result of food digestion, in quantities comparable with or exceeding the doses that are introduced as medication.…”

Section: Glycine As An Active Pharmaceutical Ingredientmentioning

confidence: 99%

Glycine: The Gift that Keeps on Giving

Boldyreva

2021

Israel Journal of Chemistry

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Glycine is a small molecule. It cannot change its conformation and is achiral. Despite the apparent simplicity, glycine shows endless diversity in its behavior over many phenomena. It was the first amino acid for which polymorphism was reported, first on crystallization and then on hydrostatic compression. The polymorphs differ in their physical properties and their biological activity. Glycine clusters persist in solution, leading to "solution memory". Phenomena at interfaces are critically important for crystal growth, dissolution, and for physical properties, which can be at times unexpected, like polarity in centrosymmetric αpolymorph. It is a great pleasure to remind of these remarkable phenomena in a special issue honoring professors Meir Lahav and Leslie Leiserowitz, who pioneered the study of the behavior of this unique molecule in many respects, and showed how complex and non-trivial phenomena can be at interfaces: between phases and between research fields.

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“…In solid state under ambient conditions, it has three polymorphs [15]: the most stable γ-glycine (γ-form), the metastable α-glycine (α-form) and the least stable β-glycine (β-form), belonging to space group P31 (or P32), P21/n and P21, respectively (refer to Table S1 in the Supplementary Materials for more properties [16][17][18] of these three polymorphs). Glycine solids have applications in treating health problems [19]. Interestingly, it was found that, compared with α-glycine, γ-glycine exerts a beneficial effect on the behavior of catalepsy-prone rats [19], highlighting the importance of controlling glycine polymorphs.…”

Section: Introductionmentioning

confidence: 99%

“…Glycine solids have applications in treating health problems [19]. Interestingly, it was found that, compared with α-glycine, γ-glycine exerts a beneficial effect on the behavior of catalepsy-prone rats [19], highlighting the importance of controlling glycine polymorphs.…”

Section: Introductionmentioning

confidence: 99%

Understanding the Salt-Dependent Outcome of Glycine Polymorphic Nucleation

Han

Tan

2021

Pharmaceutics

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The salt-dependent polymorphs of glycine crystals formed from bulk solutions have been a longstanding riddle. In this study, in order to shed fresh light, we studied the effects of seven common salts on primary nucleation of the metastable α-glycine and the stable γ-glycine. Our nucleation experiments and in-depth data analyses enabled us to reveal that (NH4)2SO4, NaCl and KNO3, in general, promote γ-glycine primary nucleation very significantly while simultaneously inhibiting α-glycine primary nucleation, thereby explaining why these three salts induce γ-glycine readily. In comparison, Ca(NO3)2 and MgSO4 also promote γ-glycine and inhibit α-glycine primary nucleation but not sufficiently to induce γ-glycine. More interestingly, Na2SO4 and K2SO4 promote not only γ-glycine but also α-glycine primary nucleation, which is unexpected and presents a rare case where a single additive promotes the nucleation of both polymorphs. As a result, the promoting effects of Na2SO4 and K2SO4 on γ-glycine do not enable γ-glycine nucleation to be more competitive than α-glycine nucleation, with γ-glycine failing to appear. These observations help us to better understand salt-governed glycine polymorphic selectivity.

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Effects of the alpha- and gamma-polymorphs of glycine on the behavior of catalepsy prone rats

Cited by 24 publications

References 37 publications

Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration

Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration

Glycine: The Gift that Keeps on Giving

Understanding the Salt-Dependent Outcome of Glycine Polymorphic Nucleation

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