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MedKoo Cat#: 558996 | Name: Picamilon
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Picamilon is a derivative of γ-aminobutyric acid (GABA). It increases parietal cortical blood flow in rats and rabbits when administered at doses of 50 mg/kg, i.p. and 10 mg/kg, i.v., respectively. Picamilon (10 mg/kg) increases latency to enter the dark compartment in the passive avoidance conditioned reflex test in rats compared with control animals, indicating nootropic effects.

Chemical Structure

Picamilon
Picamilon
CAS#34562-97-5

Theoretical Analysis

MedKoo Cat#: 558996

Name: Picamilon

CAS#: 34562-97-5

Chemical Formula: C10H12N2O3

Exact Mass: 208.0848

Molecular Weight: 208.22

Elemental Analysis: C, 57.69; H, 5.81; N, 13.45; O, 23.05

Price and Availability

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Synonym
Picamilon; Nicotinoyl-GABA; Nicotinoyl GABA;
IUPAC/Chemical Name
4-[(3-pyridinylcarbonyl)amino]-butanoic acid
InChi Key
NAJVRARAUNYNDX-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H12N2O3/c13-9(14)4-2-6-12-10(15)8-3-1-5-11-7-8/h1,3,5,7H,2,4,6H2,(H,12,15)(H,13,14)
SMILES Code
O=C(NCCCC(O)=O)C1=CN=CC=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Picamilon is a derivative of γ-aminobutyric acid that has nootropic effect.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 17.0 81.65
DMSO:PBS (pH 7.2) (1:9) 0.1 0.48
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 208.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Santillo MF, Sprando RL. Picamilon, a γ-aminobutyric acid (GABA) analogue and marketed nootropic, is inactive against 50 biological targets. Basic Clin Pharmacol Toxicol. 2023 Apr;132(4):355-358. doi: 10.1111/bcpt.13836. Epub 2023 Jan 31. PMID: 36668678. 2: Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA. Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States. Drug Test Anal. 2016 Mar- Apr;8(3-4):334-43. doi: 10.1002/dta.1853. Epub 2015 Oct 1. PMID: 26426301. 3: Cui W, Chen X, Zhan Y, Zhang Z, Zhang Y, Zhong D. Determination of picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 May 1;878(15-16):1181-4. doi: 10.1016/j.jchromb.2010.03.013. Epub 2010 Mar 16. PMID: 20359966. 4: Zakharov VV, Borodulina IV, Vakhnina NV. Lechenie bol'nykh s khronicheskoi ishemiei golovnogo mozga: opyt primeneniya kombinirovannogo neiroprotektivnogo preparata Pikamilon Ginkgo [Treatment of patients with chronic cerebral ischemia: experience of using the combined neuroprotective drug Picamilon Ginkgo]. Zh Nevrol Psikhiatr Im S S Korsakova. 2022;122(9):95-103. Russian. doi: 10.17116/jnevro202212209195. PMID: 36168693. 5: Titova NV, Bezdolny YN, Katunina EA. Asteniya, psikhicheskaya utomlyaemost' i kognitivnaya disfunktsiya [Asthenia, mental fatigue and cognitive dysfunction]. Zh Nevrol Psikhiatr Im S S Korsakova. 2023;123(5):38-47. Russian. doi: 10.17116/jnevro202312305138. PMID: 37315240. 6: Cohen PA, Avula B, Wang YH, Zakharevich I, Khan I. Five Unapproved Drugs Found in Cognitive Enhancement Supplements. Neurol Clin Pract. 2021 Jun;11(3):e303-e307. doi: 10.1212/CPJ.0000000000000960. PMID: 34484905; PMCID: PMC8382366. 7: Bugaeva LI, Spasov AA, Verovskiĭ VE, Iezhitsa IN. Doklinicheskiĭ prognoz bezopasnosti piratsetama i pikamilona na osnove pokazateleĭ ostroĭ toksichnosti [Preclinical prognosis of pyracetam and picamilon safety based on acute toxicity data]. Eksp Klin Farmakol. 2003 Jul-Aug;66(4):43-6. Russian. PMID: 14558352. 8: Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS. [Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon]. Eksp Klin Farmakol. 2005 Jan-Feb;68(1):20-4. Russian. PMID: 15786959. 9: Egorov EA, Gvetadze AA, Davydova NG. [Antioxidant agents in neuroprotection treatment of glaucoma]. Vestn Oftalmol. 2013 Mar-Apr;129(2):69-70, 73. Russian. PMID: 23808185. 10: Likhodeev VA, Spasov AA, Isupov IB, Mandrikov VB. [Effects of aminalon, fenibut, and picamilon on the typological parameters of cerebral hemodynamics in swimmers with dysadaptation syndrome]. Eksp Klin Farmakol. 2009 Jul- Aug;72(4):15-9. Russian. PMID: 19803364. 11: Dorofeev BF, Kholodov LE. Farmakokinetika pikamilona u zhivotnykh [Pikamilon pharmacokinetics in animals]. Farmakol Toksikol. 1991 Mar-Apr;54(2):66-9. Russian. PMID: 1884802. 12: Chayrov R, Volkova T, Perlovich G, Zeng L, Li Z, Štícha M, Liu R, Stankova I. Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug. Pharmaceuticals (Basel). 2022 Sep 5;15(9):1108. doi: 10.3390/ph15091108. PMID: 36145329; PMCID: PMC9500833. 13: Mirzoian RS, Gan'shina TS. Novyĭ tserebrovaskuliarnyĭ preparat pikamilon [The new cerebrovascular preparation pikamilon]. Farmakol Toksikol. 1989 Jan- Feb;52(1):23-6. Russian. PMID: 2707413. 14: Mirzoian RS. Neĭroprotektornye i tserebrovaskuliarnye éffekty GAMK-mimetikov [Neuroprotective and cerebrovascular effects of GABA mimetics]. Eksp Klin Farmakol. 2003 Mar-Apr;66(2):53-6. Russian. PMID: 12962049. 15: Kuchmerovskaia TM, Parkhomets PK, Donchenko GV, Obrosova IG, Klimenko AP, Kuchmerovskiĭ NA, Pakirbaeva LV, Efimov AS. Korrektsiia diabeticheskikh neĭropatiĭ s pomoshch'iu ingibitorov al'dozoreduktazy i pikamilona [Correction of diabetic neuropathies using aldose reductase inhibitors and pikamilon]. Vopr Med Khim. 1998 Nov-Dec;44(6):559-64. Russian. PMID: 10599142. 16: Basinskiĭ SN, Krasnogorskaia VN, Lenis IuA. Patogeneticheski orientirovannoe lechenie tsentral'nykh khorioretinal'nykh distrofiĭ s ispol'zovaniem preparata "pikamilon" [Pathogenetic treatment of central chorioretinal dystrophies with pikamilon]. Vestn Oftalmol. 2001 Mar-Apr;117(2):42-4. Russian. PMID: 11510167. 17: Logaĭ IM, Leus NF, Rozanova ZA. Osobennosti pogloshcheniia setchatkoĭ mechenykh preparatov pikamilona i GAMK [The characteristics of the retinal absorption of labelled preparations of pikamilon and GABA]. Fiziol Zh (1978). 1991 Mar-Apr;37(2):116-8. Russian. PMID: 2055321. 18: Matsuyama K, Yamashita C, Noda A, Goto S, Noda H, Ichimaru Y, Gomita Y. Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA. Chem Pharm Bull (Tokyo). 1984 Oct;32(10):4089-95. doi: 10.1248/cpb.32.4089. PMID: 6529802. 19: Egorov EA, Gvetadze AA, Vinogradova EP. [Efficacy of vision correcting system "focus" for prevention and treatment of dry form of age macular degeneration]. Vestn Oftalmol. 2012 Jan-Feb;128(1):44-6. Russian. PMID: 22741296. 20: Akopian VP, Balian LS, Zakarian NA. [Effect of nootropes on quantitative changes in the rat cerebral cortex GABA(A) receptor complexes under experimental hypokinesia conditions]. Eksp Klin Farmakol. 2010 Jul;73(7):13-5. Russian. PMID: 20821973.