Nerisopam

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

MedKoo CAT#: 528407

CAS#: 102771-12-0

Description: Nerisopam, also known as EGIS-6775 and GYKI-52322, is a gamma-aminobutyric acid (GABA) receptor agonist potentially for the treatment of anxiety and psychiatric disorders.

Chemical Structure

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Nerisopam
CAS# 102771-12-0
Instruction

Theoretical Analysis

MedKoo Cat#: 528407
Name: Nerisopam
CAS#: 102771-12-0
Chemical Formula: C18H19N3O2
Exact Mass: 309.15
Molecular Weight: 309.369
Elemental Analysis: C, 69.88; H, 6.19; N, 13.58; O, 10.34

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: Nerisopam; GYKI-52322; GYKI 52322; GYKI52322; EGIS-6775; EGIS6775; EGIS 6775

IUPAC/Chemical Name: 4-(7,8-dimethoxy-4-methyl-5H-benzo[d][1,2]diazepin-1-yl)aniline

InChi Key: WWQDEXGFYVSTCX-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H19N3O2/c1-11-8-13-9-16(22-2)17(23-3)10-15(13)18(21-20-11)12-4-6-14(19)7-5-12/h4-7,9-10H,8,19H2,1-3H3

SMILES Code: NC1=CC=C(C2=NN=C(C)CC3=CC(OC)=C(OC)C=C32)C=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: >2 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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 309.37 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:
In vitro protocol:
In vivo protocol:

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1: Minami T, Matsumura S, Nishizawa M, Sasaguri Y, Hamanaka N, Ito S. Acute and late effects on induction of allodynia by acromelic acid, a mushroom poison related structurally to kainic acid. Br J Pharmacol. 2004 Jun;142(4):679-88. PubMed PMID: 15159282; PubMed Central PMCID: PMC1575046.

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3: Horváth EJ, Salamon C, Bakonyi A, Fekete MI, Palkovits M. [(3)H]-girisopam, a novel selective benzodiazepine for the 2, 3-benzodiazepine binding site. Brain Res Brain Res Protoc. 1999 Jul;4(2):230-5. PubMed PMID: 10446419.

4: Fekete MI, Horváth K, Kedves R, Máté I, Székely JI, Szentkuti E. Selective interaction of homophtalazine derivatives with morphine. Eur J Pharmacol. 1997 Jul 23;331(2-3):175-83. PubMed PMID: 9274977.

5: Palkovits M, Baffi JS, Berzsenyi P, Horváth EJ. Anxiolytic homophthalazines increase Fos-like immunoreactivity in selected brain areas of the rat. Eur J Pharmacol. 1997 Jul 16;331(1):53-63. PubMed PMID: 9274930.

6: Róna K, Ary K, Renczes G, Gachályi B, Grézal G, Drabant S, Csörgö M, Klebovich I. [Human pharmacokinetic study of nerisopam and its n-acetyl metabolite]. Acta Pharm Hung. 1997 Mar-May;67(2-3):65-71. Hungarian. PubMed PMID: 9289938.

7: Ary K, Róna K, Renczes G, Gachályi B, Riesz T, Grézal G, Klebovich I. [Pharmacokinetic study of nerisopam and its n-acetyl metabolite in rats]. Acta Pharm Hung. 1997 Mar-May;67(2-3):59-63. Hungarian. PubMed PMID: 9289937.

8: Rona K, Ary K, Gachalyi B, Klebovich I, Tomori E. Simultaneous determination of nerisopam, a novel anxiolytic agent showing polymorphic metabolism, and its N-acetyl metabolite from human plasma by a validated high performance liquid chromatographic method. J Chromatogr B Biomed Appl. 1996 Mar 29;678(1):63-72. PubMed PMID: 8861657.

9: Horváth EJ, Palkovits M, Lenkei Z, Gyüre KI, Fekete MI, Arányi P. Autoradiographic localization and quantitative determination of specific binding sites of anxiolytic homophthalazines (formerly called 2,3-benzodiazepines) in the striato-pallido-nigral system of rats. Brain Res Mol Brain Res. 1994 Mar;22(1-4):211-8. PubMed PMID: 8015381.

10: Horváth K, Andrási F, Botka P, Hámori T. Anxiolytic profile of girisopam and GYKI 52,322 (EGIS 6775). Comparison with chlordiazepoxide and buspirone. Acta Physiol Hung. 1992;79(2):153-61. PubMed PMID: 1363928.

11: Horváth K, Andrási F, Berzsenyi P, Pátfalusi M, Patthy M, Szabó G, Sebestyén L, Bagdy E, Körösi J, Botka P, et al. A new psychoactive 5H-2,3-benzodiazepine with a unique spectrum of activity. Arzneimittelforschung. 1989 Aug;39(8):894-9. PubMed PMID: 2573361.

12: Pátfalusi M, Horváth G, Fetter I, Elekes I, Tomori E, Láng T. [Pharmacokinetics and metabolic investigations of a new, atypical analeptic (GYKI-52322)]. Acta Pharm Hung. 1989;59 Suppl 1:12-20. Hungarian. PubMed PMID: 2577097.