ORG-28611 (SCH-900,111) is a potent cannabinoid receptor full agonist, developed by Organon International for treatment pain. In preclinical studies, Org 28611 exhibited high affinity for both CB1 and CB2 cannabinoid receptors, as determined by radioligand competition binding assays and rapidly metabolized by mouse and human hepatic microsomes and showed higher total levels in the brain compared to plasma. In clinical trials, Org 28611 does not provide enough sedation for outpatient surgical procedures, does not induce anterograde amnesia and causes undesirable subjective effects at higher doses. However, bolus doses up to 3 μ/kg (with maximum initial plasma concentrations of 24 ng/mL) or mean plasma levels up to 4 ng/mL are well tolerated and make it worthwhile to further explore the analgesic or antiemetic properties.

Rapacuronium bromide (RAPLON), a nondepolarizing neuromuscular blocking agent, is a negative allosteric modulator of muscarinic acetylcholine receptors. Rapacuronium bromide is indicated as an adjunct to general anesthesia to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgical procedures. There were no specific pharmacokinetic studies conducted to examine the drug-drug interactions of RAPLON. Due to the risk of fatal bronchospasm, it was withdrawn from the United States market less than 2 years after its FDA approval.

ORG-28611 (SCH-900,111) is a potent cannabinoid receptor full agonist, developed by Organon International for treatment pain. In preclinical studies, Org 28611 exhibited high affinity for both CB1 and CB2 cannabinoid receptors, as determined by radioligand competition binding assays and rapidly metabolized by mouse and human hepatic microsomes and showed higher total levels in the brain compared to plasma. In clinical trials, Org 28611 does not provide enough sedation for outpatient surgical procedures, does not induce anterograde amnesia and causes undesirable subjective effects at higher doses. However, bolus doses up to 3 μ/kg (with maximum initial plasma concentrations of 24 ng/mL) or mean plasma levels up to 4 ng/mL are well tolerated and make it worthwhile to further explore the analgesic or antiemetic properties.

Rapacuronium bromide (RAPLON), a nondepolarizing neuromuscular blocking agent, is a negative allosteric modulator of muscarinic acetylcholine receptors. Rapacuronium bromide is indicated as an adjunct to general anesthesia to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgical procedures. There were no specific pharmacokinetic studies conducted to examine the drug-drug interactions of RAPLON. Due to the risk of fatal bronchospasm, it was withdrawn from the United States market less than 2 years after its FDA approval.