MedKoo Cat#: 592909 | Name: Apadoline
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Description:

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

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

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

Theoretical Analysis

MedKoo Cat#: 592909

Name: Apadoline

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

Chemical Formula: C23H29N3OS

Exact Mass: 395.2031

Molecular Weight: 395.57

Elemental Analysis: C, 69.84; H, 7.39; N, 10.62; O, 4.04; S, 8.10

Price and Availability

Size Price Availability Quantity
1mg USD 150.00 Ready to ship
5mg USD 350.00 Ready to ship
10mg USD 550.00 Ready to ship
25mg USD 950.00 Ready to ship
50mg USD 1,650.00 Ready to ship
100mg USD 2,950.00 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
More Info
Agonists at kappa-opioid receptors may preserve the analgesic properties of mu-opioidergic agonists while avoiding their major adverse effects.
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 395.57 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.
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.