Perlapine
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MedKoo CAT#: 523128

CAS#: 1977-11-3

Description: Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). This drug exhibits >10,000-fold selectivity for hM3Dq over hM3.

Chemical Structure

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Perlapine
CAS# 1977-11-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 523128
Name: Perlapine
CAS#: 1977-11-3
Chemical Formula: C19H21N3
Exact Mass: 291.17
Molecular Weight: 291.398
Elemental Analysis: C, 78.32; H, 7.26; N, 14.42

Price and Availability

Size Price Availability Quantity
5mg USD 190
10mg USD 350
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Synonym: Perlapine

IUPAC/Chemical Name: 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine

InChi Key: PWRPUAKXMQAFCJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H21N3/c1-21-10-12-22(13-11-21)19-17-8-4-2-6-15(17)14-16-7-3-5-9-18(16)20-19/h2-9H,10-14H2,1H3

SMILES Code: CN1CCN(C2=NC3=CC=CC=C3CC4=CC=CC=C42)CC1

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
Instruction:
View handling instruction
Biological target: Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM).
In vitro activity: From this screen, this study discovered perlapine as a novel, potent agonist of hM3Dq (Figure (Figure3).3). Importantly, perlapine was >10 000-fold selective for hM3Dq over hM3. Interestingly, perlapine contains a different tricyclic core in comparison with CNO. The high hM3Dq potency of perlapine suggests that the benzodiazepine tricyclic core of the CNO (compound 5a) scaffold is not required for maintaining high hM3Dq agonist activity. Reference: ACS Chem Neurosci. 2015 Mar 18;6(3):476-84. https://pubmed.ncbi.nlm.nih.gov/25587888/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 34.32
DMSO 12.3 42.16
DMSO:PBS (pH 7.2) (1:1) 0.5 1.72
Ethanol 5.0 17.16

Preparing Stock Solutions

The following data is based on the product molecular weight 291.40 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: Chen X, Choo H, Huang XP, Yang X, Stone O, Roth BL, Jin J. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84. doi: 10.1021/cn500325v. Epub 2015 Jan 27. PMID: 25587888; PMCID: PMC4368042.
In vitro protocol: Chen X, Choo H, Huang XP, Yang X, Stone O, Roth BL, Jin J. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84. doi: 10.1021/cn500325v. Epub 2015 Jan 27. PMID: 25587888; PMCID: PMC4368042.
In vivo protocol: TBD

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1: Meltzer HY, Fessler RG, Fang VS. Perlapine: relationship between stimulation of prolactin secretion and antipsychotic activity. Psychopharmacology (Berl). 1977 Oct 20;54(2):183-6. PubMed PMID: 412213.

2: Wilk S, Stanley M. Perlapine and dopamine metabolism: prediction of antipsychotic efficacy. Eur J Pharmacol. 1977 Jan 7;41(1):65-72. PubMed PMID: 12986.

3: Bürki HR, Ruch W, Asper H. Effects of clozapine, thioridazine, perlapine and haloperidol on the metabolism of the biogenic amines in the brain of the rat. Psychopharmacologia. 1975;41(1):27-33. PubMed PMID: 235767.

4: Allen SR, Oswald I. The effects of perlapine on sleep. Psychopharmacologia. 1973 Aug 22;32(1):1-9. PubMed PMID: 4359662.

5: Stille G, Sayers A, Lauener H, Eichenberger E. 6-(4-Methyl-1-piperazinyl)morphanthridine (Perlapine), a new tricyclic compound with sedative and sleep-promoting properties. A pharmacological study. Psychopharmacologia. 1973 Feb 20;28(4):325-37. PubMed PMID: 4695567.