GR 113808 | CAS# 144625-51-4 | 5-HT4 receptor antagonist

GR 113808
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531848

CAS#: 144625-51-4

Description: GR 113808 is a potent, selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, and Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). GR 113808 displays > 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.

Chemical Structure

GR 113808

CAS# 144625-51-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531848
Name: GR 113808
CAS#: 144625-51-4
Chemical Formula: C19H27N3O4S
Exact Mass: 393.17
Molecular Weight: 393.502
Elemental Analysis: C, 57.99; H, 6.92; N, 10.68; O, 16.26; S, 8.15

Price and Availability

Size	Price	Availability
10mg	USD 350	2 Weeks
25mg	USD 700	2 Weeks
50mg	USD 1150
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GR 113808; GR113808; GR-113808.

IUPAC/Chemical Name: [1-(2-methanesulfonamidoethyl)piperidin-4-yl]methyl 1-methylindole-3-carboxylate

InChi Key: MOZPSIXKYJUTKI-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3

SMILES Code: O=C(C1=CN(C)C2=C1C=CC=C2)OCC3CCN(CCNS(=O)(C)=O)CC3

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:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8).
In vitro activity:	Incubation with GR113808 (10.0 nM) for either 15, 30 or 60 min displaced 5-HT concentration-effect curves to the right, producing curves with EC50 values of 0.78 (0.46-1.33) μM (n = 3), 1.22 (0.79-1.88) μM (n = 3) and 0.88 (0.07-12.70) μM (n = 3) respectively (Figure 3a). Reference: Br J Pharmacol. 1994 Jan;111(1):332-8. https://pubmed.ncbi.nlm.nih.gov/8012715/
In vivo activity:	On the guinea-pig ascending colon, GR113808 (1 nM-0.1 μM) behaved as an antagonist of 5-hydroxytryptamine (5-HT)-induced contraction, producing rightward displacements of the concentration-effect curve to 5-HT and a concentration-related depression of the maximum effect. Reference: Br J Pharmacol. 1994 Jan;111(1):332-8. https://pubmed.ncbi.nlm.nih.gov/8012715/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	39.0	99.11

Preparing Stock Solutions

The following data is based on the product molecular weight 393.50 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.

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:	1. Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. Br J Pharmacol. 1994 Jan;111(1):332-8. doi: 10.1111/j.1476-5381.1994.tb14064.x. PMID: 8012715; PMCID: PMC1910004.
In vitro protocol:	1. Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. Br J Pharmacol. 1994 Jan;111(1):332-8. doi: 10.1111/j.1476-5381.1994.tb14064.x. PMID: 8012715; PMCID: PMC1910004.
In vivo protocol:	1. Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. Br J Pharmacol. 1994 Jan;111(1):332-8. doi: 10.1111/j.1476-5381.1994.tb14064.x. PMID: 8012715; PMCID: PMC1910004.

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1: Castro L, Varjão B, Silva I, Duque B, Batista A, Santana R, Luz P, Rocha MA Jr, Fregoneze JB, De Castro-e-Silva E. Effect of the intracerebroventricular administration of GR 113808, a selective 5-HT4 antagonist, on water intake during hyperosmolarity and hypovolemia. Braz J Med Biol Res. 2001 Jun;34(6):791-6. PubMed PMID: 11378670.

2: Ansanay H, Sebben M, Bockaert J, Dumuis A. Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons. Eur J Pharmacol. 1996 Mar 7;298(2):165-74. PubMed PMID: 8867105.

3: Wong EH, Reynolds GP, Bonhaus DW, Hsu S, Eglen RM. Characterization of [3H]GR 113808 binding to 5-HT4 receptors in brain tissues from patients with neurodegenerative disorders. Behav Brain Res. 1996;73(1-2):249-52. PubMed PMID: 8788512.

4: Pozzi L, Trabace L, Invernizzi R, Samanin R. Intranigral GR-113808, a selective 5-HT4 receptor antagonist, attenuates morphine-stimulated dopamine release in the rat striatum. Brain Res. 1995 Sep 18;692(1-2):265-8. PubMed PMID: 8548313.

5: Kaumann AJ. Blockade of human atrial 5-HT4 receptors by GR 113808. Br J Pharmacol. 1993 Nov;110(3):1172-4. PubMed PMID: 8298805; PubMed Central PMCID: PMC2175795.

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