Apadoline
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MedKoo CAT#: 592909

CAS#: 135003-30-4 (free base)

Description: Apadoline, also known as RP 60180, is a non-peptidic kappa-opioid receptor agonist. From the dose of 1 mg/kg i.v., RP 60180 slowed ECG frequency. This effect, which lasted for about 30 minutes post-injection, was most often seen at the higher doses. According to literature, both RP 60180 and pentazocine reduced pain-related CSSERP amplitudes by approximately 40%. Pentazocine tended to produce more side effects.

Chemical Structure

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Apadoline
CAS# 135003-30-4 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 592909
Name: Apadoline
CAS#: 135003-30-4 (free base)
Chemical Formula: C23H29N3OS
Exact Mass: 395.20
Molecular Weight: 395.565
Elemental Analysis: C, 69.84; H, 7.39; N, 10.62; O, 4.04; S, 8.10

Price and Availability

Size Price Availability Quantity
10mg USD 550 Ready to ship
25mg USD 950 Ready to ship
50mg USD 1650 Ready to ship
100mg USD 2950 Ready to ship
1mg USD 150 Ready to ship
5mg USD 350 Ready to ship
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Related CAS #: 135003-30-4 (free base), 135092-09-0 (HCl), 203937-74-0 (S-isomer),

Synonym: Apadoline; RP 60180; RP-60180; RP60180;

IUPAC/Chemical Name: 10-[(1R)-1-Methyl-2-(1-pyrrolidinyl)ethyl]-N-propyl-10H-phenothiazine-2-carboxamide

InChi Key: KXMAIWXPZGQNCR-QGZVFWFLSA-N

InChi Code: InChI=1S/C23H29N3OS/c1-3-12-24-23(27)18-10-11-22-20(15-18)26(17(2)16-25-13-6-7-14-25)19-8-4-5-9-21(19)28-22/h4-5,8-11,15,17H,3,6-7,12-14,16H2,1-2H3,(H,24,27)/t17-/m1/s1

SMILES Code: O=C(C(C=C1N2[C@H](C)CN3CCCC3)=CC=C1SC4=C2C=CC=C4)NCCC

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: 2934.99.03.00

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Apadoline, also known as RP 60180, is a non-peptidic kappa-opioid receptor agonist.
In vitro activity: TBD
In vivo activity: From the dose of 1 mg/kg i.v., RP 60180 slowed ECG frequency. This effect, which lasted for about 30 minutes post-injection, was most often seen at the higher doses. Reference: Prog Neuropsychopharmacol Biol Psychiatry. 1995 Jul;19(4):687-97. https://pubmed.ncbi.nlm.nih.gov/8588066/

Preparing Stock Solutions

The following data is based on the product molecular weight 395.565000000000000000000000000000 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: 1. Stutzmann JM, Valin A, Böhme GA, Fardin V, Garret C, Naquet R. Electrographic studies of the effects of RP 60180, a novel kappa agonist, on the photosensitive baboon Papio papio. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Jul;19(4):687-97. doi: 10.1016/0278-5846(95)00112-9. PMID: 8588066.
In vitro protocol: TBD
In vivo protocol: 1. Stutzmann JM, Valin A, Böhme GA, Fardin V, Garret C, Naquet R. Electrographic studies of the effects of RP 60180, a novel kappa agonist, on the photosensitive baboon Papio papio. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Jul;19(4):687-97. doi: 10.1016/0278-5846(95)00112-9. PMID: 8588066.

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1: Barber A, Gottschlich R. Novel developments with selective, non-peptidic kappa-opioid receptor agonists. Expert Opin Investig Drugs. 1997 Oct;6(10):1351-68. PubMed PMID: 15989506.