Methdilazine Hydrochloride | CAS#1229-35-2 | 1982-37-2

MedKoo Cat#: 318201 | Name: Methdilazine Hydrochloride

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Description:

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

Methdilazine Hydrochloride is a first-generation antihistamine with anticholinergic properties of the phenothiazine class.

Chemical Structure

Methdilazine Hydrochloride

CAS#1229-35-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 318201

Name: Methdilazine Hydrochloride

CAS#: 1229-35-2 (HCl)

Chemical Formula: C18H21ClN2S

Exact Mass:

Molecular Weight: 332.89

Elemental Analysis: C, 64.94; H, 6.36; Cl, 10.65; N, 8.42; S, 9.63

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 450.00	out of stock
200mg	USD 750.00	out of stock

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Related CAS #

1982-37-2 (free base) 1229-35-2 (HCl)

Synonym

Methdilazine Hydrochloride; METHDILAZINE HYDROCHLORIDE; Bristaline; Disyncran; Dilosyn; Methdilazine Hcl; Tacaryl hydrochloride; methdilazine;

IUPAC/Chemical Name

10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine;hydrochloride

InChi Key

IEISBKIVLDXSMZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H20N2S.ClH/c1-19-11-10-14(12-19)13-20-15-6-2-4-8-17(15)21-18-9-5-3-7-16(18)20;/h2-9,14H,10-13H2,1H3;1H

SMILES Code

CN1CCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42.Cl

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, not in water

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

Certificate of Analysis

View CoA: current batch, Lot#T7R12C06

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Methdilazine hydrochloride is an orally active antibiotic (histamine antagonist).

In vitro activity:

The growth inhibition of Escherichia coli and Staphylococcus aureus was accompanied by significant release of K+ and UV-absorbing small molecules upon exposure to methdilazine, an extensively used phenothiazine antihistamine. Reference: J Antimicrob Chemother. 1998 Jul;42(1):83-6. https://pubmed.ncbi.nlm.nih.gov/9700532/

In vivo activity:

Antinociception was assessed in male CD-1 mice by a modification of Haffner's tail-clamp procedure. The H1 blockers, including an ethylenediamine (pyrilamine), an ethanolamine (diphenhydramine), a phenothiazine (methdilazine), a piperazine (cyclizine) and an alkylamine (chlorpheniramine), all produced antinociception when given alone to mice and also caused potentiation when combined with morphine. Reference: Neuropharmacology. 1985 Jan;24(1):1-4. https://pubmed.ncbi.nlm.nih.gov/2858829/

	Solvent	mg/mL	mM	comments
Solubility
	Soluble in DMSO, not in water	0.0	100.00

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 332.89 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. Chattopadhyay D, Mukherjee T, Pal P, Saha B, Bhadra R. Altered membrane permeability as the basis of bactericidal action of methdilazine. J Antimicrob Chemother. 1998 Jul;42(1):83-6. PMID: 9700532. 2. Chattopadhyay D, Dastidar SG, Chakrabarty AN. Antimicrobial properties of methdilazine and its synergism with antibiotics and some chemotherapeutic agents. Arzneimittelforschung. 1988 Jul;38(7):869-72. PMID: 2905130. 3. Sun CL, Hui FW, Hanig JP. Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4. doi: 10.1016/0028-3908(85)90086-3. PMID: 2858829. 4. Gmerek DE, Cowan A. An animal model for preclinical screening of systemic antipruritic agents. J Pharmacol Methods. 1983 Sep;10(2):107-12. doi: 10.1016/0160-5402(83)90073-6. PMID: 6139510.

In vitro protocol:

In vivo protocol:

1. Sun CL, Hui FW, Hanig JP. Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4. doi: 10.1016/0028-3908(85)90086-3. PMID: 2858829. 2. Gmerek DE, Cowan A. An animal model for preclinical screening of systemic antipruritic agents. J Pharmacol Methods. 1983 Sep;10(2):107-12. doi: 10.1016/0160-5402(83)90073-6. PMID: 6139510.

1: Bryant R, Burger FJ, Mantle DE, Timma DL, Trenk FB, Yoder DS. Automated assay of single tablets of methdilazine and methdilazine hydrochloride. J Pharm Sci. 1973 Aug;62(8):1355-6. PubMed PMID: 4146842. 2: RAWITZ WE, MRRKSAMER D. Evaluation of methdilazine hydrochloride in therapy of alergic rhinitis. Curr Ther Res Clin Exp. 1962 Nov;4:564-7. PubMed PMID: 13990850. 3: LUBOWE II. A clinical evaluation of a new antipruritic, methdilazine hydrochloride. Curr Ther Res Clin Exp. 1962 Feb;4:64-6. PubMed PMID: 14467052. 4: FROHMAN IP. Methdilazine hydrochloride in pruritic dermatoses. Med Times. 1962 Jan;90:25-8. PubMed PMID: 13895467. 5: CRAWFORD LV, GROGAN FT. Clinical evaluation of methdilazine hydrochloride, a new antihistamine, using double-blind and placebo control. J Tn State Med Assoc. 1960 Jul;53:307-10. PubMed PMID: 13812717. 6: HOWELL CM Jr. Evaluation of methdilazine hydrochloride as an antipruritic agent. N C Med J. 1960 May;21:194-5. PubMed PMID: 14403486.