Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2

Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2

“…), did not modify the anti-nociceptive action of F-81 ( Figure 1(C) ). Even though F-81 and C-36 showed significant kappa-affinity, the obtained results are in agreement with a generally accepted fact that the anti-nociceptive effects are mainly mediated by the mu opioid receptor 32 , 38 .…”

Demographic Characteristics and Functional Performance of the Kidneys and Hearts of Patients with Acute Tramadol Toxicity

“…The absorption of tramadol and its volume of distribution (about 3 l/kg) are usually obtained by the oral route. Following a 100-mg oral dose, a peak concentration of approximately 0.3 mg/l appears after 2 h, and its therapeutic blood levels in adults range from 0.1 to 0.3 mg/l [2,7,9]. The usual therapeutic dose is 50 mg orally, 50 to 100 mg by injection, and 100 mg rectally.…”

“…Pain is encountered clinically in some cases such as cancer, chronic neuropathy, and after operations [1]. Tramadol is a synthetic, centrally acting analgesic agent which acts as an opioid agonist [2]. It is used either alone or in combination with other NSAIDs in the treatment of cases associated with pain and depression, e. g., low back pain, spinal cord injury, and postoperative pain management [3].…”

Antidepressant Drug Discovery and Development: Mechanism and Drug Design Based on Small Molecules

“…[ 190 ] Subsequently, compound 158 was obtained by the modification of 157 with trans‐4‐phenylpyrrolidine‐3‐carboxylic acid (4‐Ph‐β‐Pro) substitution at 2‐position to increase the lipophilicity. [ 191 ] In vitro studies demonstrated that compound 158 showed potent inhibitory activity for three opioid receptors with IC 50 values of 0.85, 9.06, and 27.11 × 10 −9 m for μ, δ, and κ opioid receptors, respectively. In addition, after icv administration at the dose range of 0.1–10 μg per animal in the hot‐plate test, it produced analgesic action in a dose‐dependent manner.…”